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Journal articles on the topic 'Synthesis of 5-methyltetrazole derivatives'

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Published: 5 June 2025

Last updated: 1 August 2025

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1

P., C. SARKAR, and AGARWAL S.C. "Functional Transformation of (±)-threo-Aleuritic Acid : Synthesis of 5-Methyltetrazoles." Journal of Indian Chemical Society Vol. 74, Aug 1997 (1997): 646–47. https://doi.org/10.5281/zenodo.5891991.

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Lac Processing & Product Development Division, Indian Lac Research Institute (I.C.A.R.), Namkum, Ranchi-834 010 <em>Manuscript received 2 February 1995, revised 12 April 1996, accepted 10 July 1996</em> Functional Transformation of (±)-threo-Aleuritic Acid : Synthesis of 5-Methyltetrazoles.

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2

Krečmerová, Marcela, Hubert Hřebabecký, and Antonín Holý. "Synthesis of 5-Phenylcytosine Nucleoside Derivatives." Collection of Czechoslovak Chemical Communications 61, no. 4 (1996): 645–55. http://dx.doi.org/10.1135/cccc19960645.

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Reaction of silylated 5-phenylcytosine with 1-O-acetyl-2,3,5-tri-O-benzoyl-D-ribose, catalyzed with tin tetrachloride, and subsequent methanolysis afforded 5-phenylcytidine (2). This compound reacted with thionyl chloride in acetonitrile to give cyclic sulfite 3 which on heating in dimethylformamide was converted into 2,2'-anhydro-1-(β-D-arabinofuranosyl)-5-phenylcytosine (4). Analogous reaction of compound 2 with thionyl chloride at reflux gave 5'-chloro-5'-deoxy-2',3'-cyclic sulfite 5. Its heating in dimethylformamide afforded 5'-chloro-2,2'-anhydro derivative 6, mild alkaline hydrolysis led

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3

Liu, Xin-Hua, Bao-An Song, Pinaki S. Bhadury, et al. "Novel 5-(3-(Substituted)-4,5-dihydroisoxazol-5-yl)-2-methoxyphenyl Derivatives: Synthesis and Anticancer Activity." Australian Journal of Chemistry 61, no. 11 (2008): 864. http://dx.doi.org/10.1071/ch07395.

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Thirty novel 5-(3-(substituted phenyl)-4,5-dihydroisoxazol-5-yl)-2-methoxyphenyl derivatives were synthesized and evaluated for their antitumour activity. The bioassays showed that the 2-fluorobenzoyl derivative 6ai, the 4-trifluoromethylbenzoyl derivative 6ah, and the 3-trifluoromethyl isoxazole derivatives (6ch and 6ci) were highly effective against PC-3 cells. The IC50 values of 6ah and 6ai against PC-3 cells were 1.5 and 1.8 μg mL–1, respectively.

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4

Drašar, Pavel, and Jiří Beránek. "2',3'-O-Carbonyl derivatives of 6-azauridine in the synthesis of its 5-substituted and 5'-deoxy derivatives." Collection of Czechoslovak Chemical Communications 52, no. 8 (1987): 2070–82. http://dx.doi.org/10.1135/cccc19872070.

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Preparation of 2',3'-O-carbonyl derivatives of 5'-deoxy-6-azauridine and 6-azauridine using 1,1'-carbonyldiimidazole has been elaborated. 5'-Chloro and 5'-bromo derivatives were prepared by treatment of the 5'-O-mesyl derivative with quaternary ammonium halides, 5'-chloro derivatives also by direct halogenation with thionyl chloride in hexamethylphosphortriamide or with tetrachloromethane, triphenyl phosphine, and dimethylformamide. Derivatives of 5'-bromo-6-azauridine were reduced with tributyltin hydride to 5'-deoxy-6-azauridine compounds. 6-Azauridine 2',3'-carbonate (IVa) and its 5'-deriva

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5

Evren, Asaf Evrim, Sinem Tekinkoca, and Leyla Yurttas. "Synthesis and Antimicrobial Activity of Some New N-(1H-benzimidazol-2- yl)-2-mercaptoacetamide Derivatives." Letters in Drug Design & Discovery 15, no. 2 (2018): 154–59. http://dx.doi.org/10.2174/1570180814666170619092147.

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Background: Due to multi-drug, extended-drug, and pandrug resistance phenotypes, bacterial resistance to antibiotics and fungal infections are a general health issue. Particulary, increase of fungal infections due to secondary cause of human diseases have been observed. An extensive variety of benzimidazole derivatives have been characterized for their chemotherapeutic significance. Benzimidazole derivatives have received important attention because of pharmacological significance during current years, especially antimicrobial, anti-fungal, antitubercular, antioxidant, anti-Alzheimer's disease

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6

Persson, T., A. B. Hörnfeldt, S. Gronowitz та N. G. Johansson. "Synthesis of Mimics to 5-(2″-thienyl)-2′,3′-β-Dideoxyuridine Triphosphate". Antiviral Chemistry and Chemotherapy 7, № 2 (1996): 101–7. http://dx.doi.org/10.1177/095632029600700207.

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A series of 5′-amido derivatives of 5-(2″-thienyl)-2′,3′,5′-β-trideoxyuridine were prepared. The compounds were tested for their inhibition of cellular DNA polymerase α and α HIV-RT. The succinic fumaric and maleic acid derivatives of 5-(2″-thienyl)-2′,3′,5′-β-trideoxyuridine were investigated. None of the compounds inhibited HIV-RT. The fumaric acid derivative inhibited DNA pol α with IC50 33 μg ml−1. The succinic acid derivative was about half as active with IC50 76 μg ml−1. The 5′-N-acyl derivatives also were structurally compared to the monomethyl ester of the triphosphate using the Sybyl

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7

Holý, Antonín, Joachim König, Jiří Veselý, Dieter Cech, Ivan Votruba, and Erik De Clercq. "5'-O-Alkyl-5-fluorouridines: Synthesis and biological activity." Collection of Czechoslovak Chemical Communications 52, no. 6 (1987): 1589–608. http://dx.doi.org/10.1135/cccc19871589.

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Methyl 2,3-O-isopropylidene-D-ribofuranoside (IV) was alkylated with alkyl halides in the presence of sodium hydride and the products were transformed by acid hydrolysis and glycosylation into methyl 5-O-alkyl-D-ribofuranosides VII. Benzoylation of VII followed by acetolysis afforded 1-O-acetyl-2,3-di-O-benzoyl-5-O-alkyl-D-ribofuranoses IX which on reaction with 2,4-bis(trimethylsilyloxy)pyrimidine in the presence of tin tetrachloride in acetonitrile and subsequent hydrolysis gave 5'-O-alkyl-2',3'-di-O-benzoyluridines XIa-XIe. Methanolysis of compounds XI furnished 5'-O-alkyluridines III. The

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8

Abdel-Rahman, A. A. H., E. B. Pedersen, and C. Nielsen. "Synthesis of 5-methylisocytidine derivatives." Monatshefte f�r Chemie Chemical Monthly 127, no. 4 (1996): 455–59. http://dx.doi.org/10.1007/bf00810888.

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9

Marinov, Marin. "SYNTHESIS OF AMINO DERIVATIVES OF MONOTHIO- AND DITHIO- ANALOGUES OF CYCLOHEXANESPIRO-5-HYDANTOIN." Journal scientific and applied research 2, no. 1 (2012): 66–73. http://dx.doi.org/10.46687/jsar.v2i1.45.

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This article presents methods for synthesis of 3-amino derivatives of cyclohexanespiro-5-(2-thiohydantoin) and cyclohexanespiro-5-(2,4-dithiohydantoin). It was found out that the treatment of cyclohexanespiro-5-(2-thiohydantoin) with hydrazine hydrate under different reaction conditions led to obtaining of 3-amino derivative and 2-hydrazone of the initial compound. As a result of thionation of 3-aminocyclohexanespiro-5-hydantoin with P4S10 or Lawesson’s reagent, the corresponding dithio-analogue was synthesized. The structures of the products obtained were verified by IR, 1H NMR, 13C NMR and m

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10

Abdelhamid, Abdou Osman, and A. S. Shawali. "Synthesis of Some New 2-Imino-2,3-dihydro-1,3,4-thiadiazole and Selenadiazole Derivatives." Zeitschrift für Naturforschung B 42, no. 5 (1987): 613–16. http://dx.doi.org/10.1515/znb-1987-0516.

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(2)Diazotized 3(5)amino-5(3)-phenylpyrazole reacts with phenacylthiocyanate (1) and phenacylselenocyanate (10) to give the corresponding 1,3,4-thiadiazoline derivative (5) and 1,3,4- selenadiazoline derivative (12), respectively. A mechanism is proposed and it is substantiated by an alternate synthesis of 5 and 12 from the corresponding hydrazidoyl bromide (6) with potassium thiocyanate and potassium selenocyanate, respectively. The thiadiazoline (5) and selenadiazoline (12) give the respective N-acyl derivatives (7a) and (12) with acetic anhydride. Nitrosation of 5 and 12 gives the correspond

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11

Fatma A M Mohamed, Fatma A. M. Mohamed, Bi Bi Zainab Mazhari Bi Bi Zainab Mazhari, Mona F. Warrad Mona F Warrad, Hesham A. M. Gomaa Hesham A M Gomaa, Asmaa T. Ali Asmaa T Ali, and Shaimaa Salah Eldeen Hussein and Hendawy Om Shaimaa Salah Eldeen Hussein and Hendawy Om. "Synthesis, Characterization, Antimicrobial and Anticarcinogenic Activity of Quinazoline Derivatives." Journal of the chemical society of pakistan 45, no. 3 (2023): 256. http://dx.doi.org/10.52568/001246/jcsp/45.03.2023.

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The reaction of β-dicarbonyl compounds as ethyl acetoacetate with hydrazines is a well-established route for the creation of pyrazole derivatives. In this research, 4-hydrazinoquinazoline (4) reacted with ethyl acetoacetate in boiling ethanol it gives ethyl 3-oxobutanoate quinazolin-4-yl-hydrazone (5). Cyclization of the compound (5) in the presence of glacial acetic acid is passed to form 4-(5-hydroxy-3-methyl-1H-pyrazol-1-yl)quinazoline(6). Furthermore, the reaction of phenylisothiocyanate compounds with hydrazines is a well-established way for the synthesis of tetrazinoquinazoline (8). The

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12

Sultan Alwan, Ensaf, and Rafat Milad Mohareb. "Synthesis of bioactive heterocyclic compounds using camphor." Bulletin of the Chemical Society of Ethiopia 38, no. 4 (2024): 1069–76. http://dx.doi.org/10.4314/bcse.v38i4.20.

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The aim of the work was to synthesize novel heterocyclic compounds derived from camphor with antibacterial activity. The pyridazine, xanthene, pyranothiazole, pyridinothiazole, thiophene and pyrazole derivatives were produced from 4,11,11-trimethyl-9-phenyl-7-(2-phenylhydrazono)-3,4,5,6,7,9-hexahydro-1H-1,4-methanoxanthen-8(2H)-one (1). Thiophene derivatives 6a,b were produced according to the Gewald’s reaction for thiophene synthesis. On the other hand, pyranothiazol derivatives 8a,b were synthesized by the multicomponent reactions between xanthene derivative 5, benzaldehyde and ethylcyanoace

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13

Aesha F SH Abdassalam, Aesha F. SH Abdassalam, Semih Kurban Semih Kurban, and Nahide Gulsah Deniz and Cigdem Sayil Nahide Gulsah Deniz and Cigdem Sayil. "Synthesis and Characterization of New Naphtho- and Tetracyclic Diazaquinone Derivatives." Journal of the chemical society of pakistan 41, no. 5 (2019): 834. http://dx.doi.org/10.52568/000805/jcsp/41.05.2019.

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In this study, new 1,4-naphtho- and 5-nitro-1,4-naphtho derivatives containing N- and N,N-substituted groups which has not been reported yet, have been synthesized from 2,3-dichloronaphthalene-1,4-diones (1,9). Compounds of 2-choloro-3-((2,4,6-triflorophenyl)amino)naphthalene-1,4-dione (3) and 2-chloro-3-((4-florophenyl)amino)naphtalene-1,4-dione (7) were obtained by reactions of 2,3-dichloronaphthalene-1,4-dione 1 with 4-fluoroaniline (6) and 2,4,6-trifloroaniline (2), respectively involving a Michael addition. We reported the cyclization reactions of compounds 1 to benzo[g]pirido[3,2-b]quino

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14

Gakovic, Andrea, Maja Djurendic-Brenesel, Evgenija Djurendic, Katarina Penov-Gasi, and Marija Sakac. "Synthesis of some 16,17-secoandrost-5-ene derivatives." Chemical Industry 64, no. 2 (2010): 81–84. http://dx.doi.org/10.2298/hemind100212009g.

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Starting from 3?-acetoxy-17-oxo-16,17-secoandrost-5-ene-16-nitrile (1), 3?-acetoxy-16,17-secoandrost-5-ene-16-nitrile (4) was synthesized by a three-stage procedure. First, the formyl group of compound 1 was reduced, to yield the alcohol 2. Compound 2 was further transformed to the mesyloxy derivative 3, whose reduction with NaBH3CN gave compound 4. Apart from compound 4 as the main reaction product, two additional products were obtained, for which the GC/MS analysis suggested that they are 8(14) and 14 derivatives of compound 4. Compound 4 was transformed into 3?-hydroxy-16,17-sesoandrost-5-e

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15

Al-Harbi, Reem A. K. "Synthesis of New Coumarin Scaffold Bearing 2-Iminochromene Moiety." Acta Chimica Slovenica 70, no. 3 (2023): 380–84. http://dx.doi.org/10.17344/acsi.2023.8016.

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Coumarin is classified as one of interesting therapeutic starting research points to obtain remarkable compounds with high efficacy. So, during this research, new 2-iminochromene derivatives bearing coumarin moiety were synthesized. At first, cyanoacetohydrazone of 3-acetylcoumarin was prepared and used as the starting material. The 2-iminochromene derivatives were synthesized through the ring closure of cyanoacetohydrazone derivative with 4-hydroxysalicylaldehyde, 5-aryldiazosalicylaldehydes, 2-hydroxynaphthaldehyde and 7-hydroxychromone-6-carboxaldehyde derivative. All of the newly synthesiz

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16

C., P. SINGH. "Synthesis of N1-(2-Pyridinecarbony 1)-3-methyl-4(substituted-hydrazono)-2-pyrazolin-5-one." Journal of Indian Chemical Society Vol. 62, Mar 1985 (1985): 222–23. https://doi.org/10.5281/zenodo.6322071.

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Chemical Laboratories, Sahu Jain College, Najibabad-248 763 <em>Manuscript received 27 </em>April <em>1981, accepted 25 February 1985</em> 2-Pyridinecarboxylic acid hydrazide and their derivatives are generally used as antibacterial agent. N<sup>1</sup>-(2-Pyridinecarbonyl)-3-methyl-4-substituted hydrazono)-2-pyrazolin-5-one and their derivatives have been synthesised. Their Rf values, chemical analysis, it and nmr spectra are recorded.

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17

Wang, Jin, Teng-huo-sheng Liao, and Jian Yang. "Efficient synthesis of 2,3-dimethoxy-5-methyl-6-morpholinomethyl-1,4-benzoquinone hydrochloride." Zeitschrift für Naturforschung B 70, no. 4 (2015): 221–23. http://dx.doi.org/10.1515/znb-2014-0208.

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AbstractThe title compound (5) was prepared by a reaction sequence starting from 2,3,4,5-tetramethoxytoluene (1) via the Blanc reaction, oxidation and alkylation. The described method provides a good yield of the C-6 heterocyclic-substituted benzoquinone derivative and is suitable for the synthesis of other benzoquinone derivatives.

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18

Journal, Baghdad Science. "Synthesis and Characterization of New Heterocyclic Compounds from 2, 5- dimercapto -1, 3, 4-Thiadiazole and Their Resins." Baghdad Science Journal 13, no. 2 (2016): 275–88. http://dx.doi.org/10.21123/bsj.13.2.275-288.

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In this research, a new 1, 3, 4-Thiadiazole derivatives have been synthesized by many heterocyclic reactions. Starting from (2, 5 – dimercapto -1, 3, 4-Thiadiazole) a variety of derivatives have been synthesis. Compound (1) was synthesized by the reaction of hydrazine hydrate with carbon disulphide in absolute ethanol. The compound (1) was reacted with 1, 2-dibromoethane in presence of alkali ethanol to give the compound (2). The compound (3) was formed from the reaction of compound (2) with hydrazine hydrate. Schiff base (4) was obtained by reacting of compound (3) with the compound (p-hydrox

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19

Harada, Kazuo, and Leslie E. Orgel. "Synthesis of 5′-Deoxy-5′-nucleosideacetic Acid Derivatives." Nucleosides and Nucleotides 9, no. 6 (1990): 771–85. http://dx.doi.org/10.1080/15257779008043143.

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20

Ammar Ferman Abbood, Ahmed M. Abdula, and Younis Baqi. "New Benzimidazoles Bearin 2-Pyrazoline Moiety: Synthesis and Antimicrobial Activity." Journal of Wasit for Science and Medicine 14, no. 3 (2023): 1–12. http://dx.doi.org/10.31185/jwsm.401.

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A new series of 5-(1H-Benzimidazol-2-yl)-4,5-dihydro-1H-pyrazol-3-yl] derivatives (1-9) were synthesized and characterized using spectral analysis. The first step includes the reaction of benzimidazole-2-carboxaldehyde with the o,p-aminoacetophenone to obtain the chalcone derivative (1, 2). The cyclization reaction of chalcone by the hydrazine hydrate afforded compound (3, 4), which represents the starting material for Schiff base derivatives. New Schiff bases (5-6) were synthesized from the reaction of benzimidazole derivative (2) with the corresponding benzaldehydes. The azetidin-2-one (7) a

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21

Mohamed, Mosaad, Samir Awad, and Naglaa Ahmed. "Synthesis and antimicrobial evaluation of some 6-aryl-5-cyano-2-thiouracil derivatives." Acta Pharmaceutica 61, no. 2 (2011): 171–85. http://dx.doi.org/10.2478/v10007-011-0019-1.

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Synthesis and antimicrobial evaluation of some 6-aryl-5-cyano-2-thiouracil derivativesA series of 6-aryl-5-cyano-2-thiouracil derivatives (1a-d) was synthesized by the reaction of ethyl cyanoacetate with thiourea and aldehydes. These products were used as intermediate compounds for the synthesis of a number of thiouracil derivatives (2a-dto10a-d). All compounds were screened for antibacterial and antifungal activities. Some of the prepared compounds, 6-(4-fluorophenyl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide (2a), 4-oxo-2-thioxo-6-(3,4,5-trimethoxyphenyl)-1,2,3,4-tetrahydropy

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22

Saadi, Lina, and Shaimaa Adnan. "Synthesis, Antibacterial and Antioxidant Evaluation of 2-Substituted-4-arylidene-5(4<i>H</i>)-oxazolone Derivatives." Indonesian Journal of Chemistry 23, no. 5 (2023): 1463. http://dx.doi.org/10.22146/ijc.83052.

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In this research, the synthesis of new substituted oxazolone derivatives is described via Erlenmeyer synthesis of N-acyl amino acid. Firstly, the azo derivative 1 was prepared by coupling the diazonium salt of 3-amino-4-methoxybenzoic acid with 4,5-dichloroimidazole in sodium hydroxide solution. Benzoyl chloride derivative 2, the key intermediate of the synthesis, was synthesized by the acylation of azo-carboxylic acid derivative 1 with thionyl chloride. The resulting acyl chloride derivative reacted with glycine in a basic catalyst to form a hippuric acid derivative 3. After that, oxazolone d

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23

Konečný, Václav, Jozefína Žúžiová, Štefan Kováč, and Tibor Liptaj. "Synthesis of Novel 4-Amino-5-(disubstituted amino)-2-phenyl-2H-pyridazin-3-ones." Collection of Czechoslovak Chemical Communications 62, no. 5 (1997): 800–808. http://dx.doi.org/10.1135/cccc19970800.

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Substituted 4-amino-2-phenyl-2H-pyridazin-3-ones 5a-5j have been prepared from 4-amino-5-chloro-2-phenyl-2H-pyridazin-3-one 1 which on reactions with acetyl chloride or acetic anhydride gives 4-acetylamino derivative 2 or 4-diacetylamino derivative 3, respectively. Derivatives 2 and 3 with dialkylamines and cyclic amines yielded appropriate 4-acetylamino-5-(disubstituted amino)-2-phenyl-2H-pyridazin-3-ones 4a-4j. Subsequent alkaline hydrolysis of the acetylamino derivatives 4a-4j let to the title compounds 5a-5j, which were screened for pesticidal activity, but none of them reached activity of

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24

Mistry, Rakesh N., and K. R. Desai. "Studies on Synthesis of Some Novel Heterocyclic Azlactone Derivatives and Imidazolinone Derivatives and their Antimicrobial Activity." E-Journal of Chemistry 2, no. 1 (2005): 42–51. http://dx.doi.org/10.1155/2005/542938.

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p- Methyl benzoic acid on reaction with phosphorus pentachloride gives p - methyl benzoyl chloride derivative which on condensation with glycine gives p - methyl benzoyl glycine derivative. Now, this p - methyl benzoyl glycine derivative on condensation with various substituted aldehydes gives corresponding substituted 4 - [aryl methylidine] - 2 - [p - methyl phenyl] - oxazole - 5 - one derivatives [1(a-j)]. Further, these derivatives [1(a-j)] on condensation with 4 , 4’ - diamino diphenyl sulphone gives corresponding substituted imidazolinone - dibenzsulphone derivatives [2(a-j)], on condensa

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25

Arpan, Jadav *. and Sandip Singh. "SYNTHESIS OF NEW PYRIMIDINE DERIVATIVES AS POTENTIAL ANTICANCER AGENT." INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES 05, no. 04 (2018): 2990–95. https://doi.org/10.5281/zenodo.1231060.

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We have tried to synthesize a series of 5 derivatives of Pyrimidine. Synthesis was carried out according to reactions shown in Reaction Scheme. At first, 4th position of 2,4 dichloropyrimidne was substituted by Anthranilic acid to form Synthesis of 2-(2- chloropyrimidin-4-ylamino)benzoic acid 1[C]. 5amino-1,3,4-thiadiazole 2[B] was prepared using Synthesis of 2-(2-chloropyrimidin-4ylamino)benzoic acid 1[C] and Thiosemicarbazide as starting material. Further confirmation was carried out by IR which showed the presence of amino (-NH2) band ~3422.80 cm-1, 1H NMR spectra which revealed all the cor

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26

Shakeel Ahmed, Shiza Murad, Iqra Munir, et al. "Spectroscopic Investigation and Synthesis of N-Ethyl-5-Tolyloxymethyl Triazole Derivatives." Indus Journal of Bioscience Research 3, no. 5 (2025): 288–96. https://doi.org/10.70749/ijbr.v3i5.1234.

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High-nitrogen heterocycles' synthesis has attracted much interest because of their wide applicability in many different sectors. As a significant class of organic compounds, triazoles and their fused derivatives have emerged among these. A new triazole derivative, 4-ethyl-3-ethylthio-5-(p-tolyloxymethyl)-4H-1, 2, 4-triazole, is the subject of this work on synthesis and spectrum characterization. Ethyl 2-p-tolyloxy acetate is synthesized by reacting 3, 4-dimethoxyphenylacetic acid with ethanol under concentrated H2SO4, starting the process. The ester product is subsequently transformed into 2-p

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27

Holý, Antonín, Ivan Rosenberg, and Hana Dvořáková. "Synthesis of (3-hydroxy-2-phosphonylmethoxypropyl) derivatives of heterocyclic bases." Collection of Czechoslovak Chemical Communications 54, no. 9 (1989): 2470–501. http://dx.doi.org/10.1135/cccc19892470.

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Analogs of the antiviral 9-(S)-(3-hydroxy-2-phosphonylmethoxypropyl)adenine (HPMPA, I), containing modified heterocyclic base, were prepared from racemic or (S)-N-(2,3-dihydroxypropyl) derivatives II. Compounds II are heated with chloromethylphosphonyl dichloride (XVII), the formed chloromethylphosphonylester chlorides of compounds II react with water to give a mixture of 2'- and 3'-chloromethylphosphonyl derivatives XVIII and XIX, respectively, which on isomerization by boiling with water in the arising acidic medium affords predominantly the 3'-isomer XIX. Treatment of this isomeric mixture

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28

Murat Saracoglu, Murat Saracoglu, Zulbiye Kokbudak Zulbiye Kokbudak, and M. Izzettin Yilmazer and Fatma Kandemirli M Izzettin Yilmazer and Fatma Kandemirli. "Synthesis and DFT Studies of Pyrimidin-1(2H)-ylaminofumarate Derivatives." Journal of the chemical society of pakistan 42, no. 5 (2020): 746. http://dx.doi.org/10.52568/000679.

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Pyrimidine derivatives have biological and pharmacological properties. Therefore, in this study we focused on the synthesis various Pyrimidine derivatives to make noteworthy contributions this class of heterocyclic compounds. In the present study, the new compounds (4-6) were obtained by the reactions of 1-amino-5-benzoyl-4-phenylpyrimidin-2(1H)-one (1), 1-amino-5-(4-methylbenzoyl)-4-(4-methylphenyl)pyrimidin-2(1H)-one (2) and 1-amino-5-(4-methoxybenzoyl)-4-(4-methoxyphenyl)pyrimidin-2(1H)-one (3) with dimethyl acetylenedicarboxylate. The structures of these compounds were proved by elemental

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29

Murat Saracoglu, Murat Saracoglu, Zulbiye Kokbudak Zulbiye Kokbudak, and M. Izzettin Yilmazer and Fatma Kandemirli M Izzettin Yilmazer and Fatma Kandemirli. "Synthesis and DFT Studies of Pyrimidin-1(2H)-ylaminofumarate Derivatives." Journal of the chemical society of pakistan 42, no. 5 (2020): 746. http://dx.doi.org/10.52568/000679/jcsp/42.05.2020.

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Pyrimidine derivatives have biological and pharmacological properties. Therefore, in this study we focused on the synthesis various Pyrimidine derivatives to make noteworthy contributions this class of heterocyclic compounds. In the present study, the new compounds (4-6) were obtained by the reactions of 1-amino-5-benzoyl-4-phenylpyrimidin-2(1H)-one (1), 1-amino-5-(4-methylbenzoyl)-4-(4-methylphenyl)pyrimidin-2(1H)-one (2) and 1-amino-5-(4-methoxybenzoyl)-4-(4-methoxyphenyl)pyrimidin-2(1H)-one (3) with dimethyl acetylenedicarboxylate. The structures of these compounds were proved by elemental

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30

K., D. Patel, D. Mistry B., and R. Desai K. "Synthesis and antimicrobial activity of 2-aryl-3-[3' -(2" ,4" ,6" -trichlorophenoxymethyl)- 5' -mercapto-1' ,2' ,4' -triazol-4' -yl]-5-substituted-4-thiazolidinones." Journal of Indian Chemical Society Vol. 83, Jan 2006 (2006): 94–96. https://doi.org/10.5281/zenodo.5816502.

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Department of Chemistry, B. K. M. Science College, Valsad-396 001, Gujarat. India <em>Manuscript received 7 January 2005. revised 12 July 2005. accepted 9 September 2005</em> Some new 4-thiazolidinones derivatives have been prepared and evaluated for antibacterial activity. Characterization was made with elemental analysis. IR, NMR and muss spectral studies.

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K., P. Suhasini, Christopher V., Rama Mohana Rao S., Praveen Kumar Ch., and L. N. Murthy Y. "Synthesis, characterisation and antitubercular screening of 5(4H)-oxazolone derivatives." Journal of Indian Chemical Society Vol. 92, Jun 2015 (2015): 951–55. https://doi.org/10.5281/zenodo.5674257.

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Department of Organic Chemistry, Andhra University, Visakhapatnam-530 003, Andhra Pradesh, India <em>E-mail</em> : suhasini.kl@gmail.com, murthyyln@gmail.com Bio-Organic Chemistry Division, Indian Institute of Integrative Medicine, Jammu-180 001, J & K, India In search of new antitubercular agents, a new series of 4-(substituted benzylidene)-2-<em>p</em>-tolyloxazol-5(<em>4H</em>)-ones (5a-h) has been designed, synthesized and subjected to evaluate their antitubercular activity for the first time against <em>Mycobacterium tuberculosis</em> H37Rv, in comparison with standard drugs Rifampici

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Abdel-Rahman, Adel A. H., and Takeshi Wada. "Synthesis and Antiviral Evaluation of 5-(1,2,3-Triazol-1-ylmethyl)- uridine Derivatives." Zeitschrift für Naturforschung C 64, no. 3-4 (2009): 163–66. http://dx.doi.org/10.1515/znc-2009-3-402.

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Some 5-(1,2,3-triazol-1-ylmethyl)uridine derivatives were synthesized via the 1,3-dipolar cycloaddition of a 5-azidomethyluridine derivative with substituted acetylenes. The antiviral activities of these compounds against hepatitis A virus (HAV, MBB cell culture-adapted strain) and Herpes simplex virus type-1 (HSV-1) were tested.

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Puspaningtyas, Ayik Rosita, and Ika Oktavianawati. "Synthesis of Novel Ester-Based 5-Fluorouracil Derivatives." Jurnal Kimia Sains dan Aplikasi 27, no. 8 (2024): 354–62. http://dx.doi.org/10.14710/jksa.27.8.354-362.

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Fluorouracil (5-Fu, 1) is an antimetabolite cancer drug and the first-line drug of anticancer administration by WHO that has been widely used worldwide for more than 50 years. The development of 5-fluorouracil is an effort to obtain higher activity, decrease side effects, and create a specific target receptor compared to 5-fluorouracil. In this research, a series of novel 5-Fluorouracil (5-Fu) derivatives has been synthesized based on a benzoylation reaction (Schotten-Baumann reaction) of N1-hydroxylated 5-Fu called compound 2, 5-fluoro-1-(hydroxymethyl)-uracil. The benzoyl chloride substituen

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34

Černý, Ivan, Vladimír Pouzar, Miloš Buděšínský, Pavel Drašar та Miroslav Havel. "Epimeric 17-hydroxy derivatives of 14β-androst-5-en-3β-yl acetate". Collection of Czechoslovak Chemical Communications 55, № 10 (1990): 2510–20. http://dx.doi.org/10.1135/cccc19902510.

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A new, six-step synthesis of 3β-hydroxy-14β-androst-5-en-17-one (IX) starting from 3β-hydroxyandrost-5-en-17-one has been elaborated. Reduction of acetate X with sodium borohydride afforded 17α-hydroxy-14β-androst-5-en-3β-yl acetate (XI). The corresponding 17β-derivative XIV was obtained by epimerization of 17α-O-tosyl derivative XIII with sodium nitrite in hexamethylphosphoramide. The 13C and 1H NMR spectra of 14β-androstane derivatives are discussed.

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35

Stolarczyk, Marcin, Agnieszka Matera-Witkiewicz, Aleksandra Wolska, et al. "Synthesis, Crystal Structure, and Biological Evaluation of Novel 5-Hydroxymethylpyrimidines." Materials 14, no. 22 (2021): 6916. http://dx.doi.org/10.3390/ma14226916.

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Pyrimidine displays a wide array of bioactivities, and thence, it is still considered a potent unit of new drug research. Its derivative, 5-hydroxymethylpyrimidine, can be found as a scaffold of nontypical nitrogen bases in DNA and as a core of some natural bioactive compounds. In this study, we obtained a series of 5-hydroxymethylpyrimidines that vary in the 4-position by the reduction of proper esters. All compounds were characterized by spectroscopic analysis, and single-crystal X-ray diffraction was performed for some of them. Biological investigations estimated cytotoxic properties agains

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Hanna, Naeem B., Milena Masojídková, and Alois Pískala. "Synthesis and Biological Activity of N4-Methyl-5-azacytidines." Collection of Czechoslovak Chemical Communications 63, no. 5 (1998): 713–22. http://dx.doi.org/10.1135/cccc19980713.

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Protected N4-methyl and N4,N4-dimethyl derivatives of 5-azacytidine 3 and 4 were prepared by selective aminolysis of benzoylated 4-methoxy-1-(β-D-ribofuranosyl)-1,3,5-triazin-2(1H)-one 5, by glycosylation of silylated N4-methyl- or N4,N4-dimethyl-5-azacytosines 7 and 8 with 2,3,5-tri-O-benzoyl-α,β-D-ribofuranosyl chloride (11) or by several modifications of the isocyanate method. By the isocyanate approach, also the α-D anomer of protected N4-methyl-5-azacytidine 17 was obtained as a minor product. The protected dimethyl derivative 4 was also obtained by the reaction of isobiuret 22 with dimet

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Mistry, Rakesh N., and K. R. Desai. "Studies on Synthesis of Some Novel Heterocyclic Chalcone, Pyrazoline, Pyrimidine - 2 - One, Pyrimidine - 2 - Thione,para-Acetanilide Sulphonyl and Benzoyl Derivatives and their Antimicrobial Activity." E-Journal of Chemistry 2, no. 1 (2005): 30–41. http://dx.doi.org/10.1155/2005/953107.

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1, 2 - Dichloro benzene on chlorosulphonation by chlorosulphonic acid gives 1, 2 - [dichloro] - benzene sulphonyl chloride which on condensation withp–amino acetophenone gives 1-[acetyl] - 1’ , 2’ - [dichloro] - dibenz sulphonamide derivative. This derivative undergo condensation with 2,4- dichloro benzaldehyde gives 1- [3” - (sub. phenyl) - 2” - propene - 1” - one] - 1’ , 2’ - [dichloro] - dibenz sulphonamide derivative which on reaction with 99% hydrazine hydrate and glacial acetic acid gives 1-[acetyl]-3- [1’ , 2’ - (dichloro) - dibenz sulphonamide] -5 - [2” , 4” - dichloro phenyl] - 2 - py

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38

Musin, A. I., Yu G. Borisova, Sh Sh Dzhumaev, et al. "Synthesis and biological activity of 5-acetyl- and 5-hydroxyalkyl1,3-dioxane derivatives." Fine Chemical Technologies 18, no. 4 (2023): 381–91. http://dx.doi.org/10.32362/2410-6593-2023-18-4-381-391.

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Objectives. To synthesize derivatives of 5-acetyl- and 5-hydroxyalkyl-1,3-dioxanes and evaluate their effect on platelet aggregation and plasma hemostasis.Methods. To determine the qualitative and quantitative composition of the reaction masses, gas chromatography-, chromate mass spectrometry-, and 1H and 13C nuclear magnetic resonance spectrometry methods were used.Results. Derivatives of 5-acetyl- and 5-hydroxyalkyl-1,3-dioxanes were obtained under thermal heating conditions in order to evaluate their effect on platelet aggregation and plasma hemostasis.Conclusions. Derivatives of 5-acetyl-

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Ahmed, H. Shamroukh, E. Rashad Aymn, T. Gaballah Samir, A. A. Osman Dalia, I. Hashem Ahmed, and M. E. Abdel-Megeid Farouk. "Synthesis of some N-Acyclic Pyrazolopyrimidine Nucleosides and Pyrazolotriazolopyrimidines." Chemistry Research Journal 5, no. 5 (2020): 89–96. https://doi.org/10.5281/zenodo.13144550.

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<strong>Abstract </strong>Pyrazolo[3,4-<em>d</em>]pyrimidin-4-one derivative <strong>1</strong> was used as a key compound for the preparation of some <em>N</em>-acyclic nucleosides of pyrazolo[3,4-<em>d</em>]pyrimidines <strong>2-5</strong>. Also, the synthesis and structure characterization of pyrazolo[3,4-<em>d</em>]pyrimidin-6-yl-hydrazine derivative <strong>6 </strong>was reported as a key compound for the preparation of pyrazolotriazolopyrimidine derivatives <strong>7</strong>-<strong>9 </strong>under different suitable reaction conditions. Cyclization of the hydrazone derivatives <stron

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40

Khalifa, Nagy M., Ahmed M. Naglah, Mohamed A. Al-Omara, and Abd El-Galil E. Amr. "Synthesis and Reactions of New Chiral Linear Dipeptide Candidates Using Nalidixic Acid as Starting Material." Zeitschrift für Naturforschung B 69, no. 6 (2014): 728–36. http://dx.doi.org/10.5560/znb.2014-4031.

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A series of dipeptide heterocyclic derivatives 4-15 were synthesized using methyl 2-{[(1-ethyl- 7-methyl-4-oxo-1,4-dihydro-1,8-naphthyridin-3-yl)carbonyl]amino}-3-ethylbutanoate (3) as starting material. Treatment of 3 with L-phenylalanine methyl ester hydrochloride afforded the corresponding dipeptide methyl ester derivative 4, which was treated with hydrazine hydrate to afford the dipeptide acid hydrazide 5. Compound 5 was coupled with aldehyde and acetophenone derivatives to afford the corresponding Schiff bases 6a-f. The hydrazide derivative 5 was reacted with ethyl acetoacetate or acetone

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41

Zhang, Hao, Yanbang Li, and Liangbing Gan. "Selective Synthesis of [60]Fullerene Multiadducts through Dicyclohexylcarbodiimide (DCC) Mediated Reactions." Synlett 29, no. 09 (2018): 1167–70. http://dx.doi.org/10.1055/s-0036-1591770.

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4-Methylpiperidine (MePi) reacts with C60 in the presence of DCC to form C60(MePi)4(DCC). The DCC moiety in the C60 derivative facilitates facile replacement reactions with thiols and phenols to form pentathiolyl derivatives C60(RS)5(H) and benzofuran-containing C60 derivatives such as C60(MePi)2(OC6H4), respectively.

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42

Shao, Jiaan, Wenteng Chen, Di Ke, Ke Shu, En Chen, and Yongping Yu. "Highly Efficient Synthesis of Polysubstituted 2-Aminopyrroles via a Multicomponent Domino Reaction." Synlett 29, no. 07 (2018): 922–27. http://dx.doi.org/10.1055/s-0036-1591907.

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A highly efficient approach to polysubstituted 2-aminopyrroles containing a coumarin derivative unit at the 5-position of the pyrrole ring was developed via a novel multicomponent domino reaction of glyoxal monohydrate derivatives, anilines, coumarin derivatives, and malononitrile. This transformation proceeded via an α-aminoketone as the key intermediate.

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43

Thanki, Pragna H., Dhaval V. Hingrajiya, Jayesh J. Modha, and Jalpa H. Vadgama. "Synthesis, characterization and antibiotic evaluation of various biologically active derivatives of 4-Alkylpyrimidine-5-carbonitrile." Current Chemistry Letters 12, no. 3 (2023): 537–44. http://dx.doi.org/10.5267/j.ccl.2023.3.002.

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Extensive research work has been published on Tetrahydro and Dihydropyrimidine derivatives. Pyrimidine-5-Carbonitrile and its analogs have demonstrated a large number of activities. Some 6-Halogenosubstituted pyrimidine analogs have also been reported to be biologically active to a certain extent, but the literature survey reveals not much report on 6-alkylated pyrimidine derivatives. Targeting enhancement in biologically useful properties of a lead molecule through the association of it with active pharmacophoric groups or molecules is a conventional method in pharmaceutical research. With an

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44

K., Ramaiah, S. Grossert J, L. Hooper D., K. Dubey P., and Ramanatham J. "Studies on synthesis of 2-acetylbenzimidazole and related benzimidazole derivatives." Journal of Indian Chemical Society Vol. 76, Mar 1999 (1999): 140–44. https://doi.org/10.5281/zenodo.5853398.

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Department of Chemistry, College of Engineering, J. N. T. University, Kukatpally, Hyderabad-500 072, India Department of Chemistry, Dalhousie University, Halifax, N.S., B3H 4J3, Canada <em>Munuscript received 10 February 1998, revised 7 August 1998, accepted 18 November 1998</em> Condensation of a-phenylenediamine (1) with propanoic acid under Phillips' conditions gives 2-ethylbenzimidazole (2). Attempts to oxidise 2 to 2-acetylbenzimidazolc (3) using H<sub>2</sub>O<sub>2</sub>, SeO<sub>2</sub>, KMnO<sub>4</sub> acetonc were unsuccessful. Condensation of 2 with benzaldehyde yields 2-(

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45

Jachak, Madhukar, Martin Mittelbach, and Hans Junek. "Synthesis with Nitriles: 92. Synthesis of 5-Formylcytosine Derivatives." HETEROCYCLES 36, no. 10 (1993): 2281. http://dx.doi.org/10.3987/com-93-6416.

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46

Harnden, MR, and DT Hurst. "The Chemistry of Pyrimidinethiols. III. The Synthesis of Some Substituted Pyrimidinthiols and Some Thiazolo[5,4-D]pyrimidines." Australian Journal of Chemistry 43, no. 1 (1990): 55. http://dx.doi.org/10.1071/ch9900055.

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The preparation of a number of pyrimidinethiols and (substituted) thiopyrimidines has been carried out. The reaction of 5-acetylamino-2-aminopyrimidine-4,6-diol with phosphorus penta -sulfide in pyridine gave 5-amino-2-methylthiazolo[5,4-d]pyrimidine-7-thiol which was used to prepare several additional novel pyrimidine derivatives. Hydrolysis of the 4-carboxymethylthio derivative by using 5M hydrochloric acid gave 2,5-diamino-6-mercaptopyrimidin-4-ol hy -drochloride whilst hydrolysis of 2-methyl-7-methylthiothiazolo[5,4-d]pyrimidin-5-amine gave the corresponding 4-hydroxy derivative. Several 4

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47

Jaiswal, Dr Shalini. "PTSA Catalysed Expeditious Synthesis and Antimicrobial Activities of Dihydro-3, 5-Diphenylisoxazole Derivatives." Global Journal For Research Analysis 3, no. 7 (2012): 214–15. http://dx.doi.org/10.15373/22778160/july2014/77.

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48

Ameen, Ban, ASMAA Jawad, and Evon Akram. "Synthesis, In Vitro Biological Activity and Anti-Breast Cancer of Diazepine Derivatives." Al-Kufa University Journal for Biology 16, no. 3 (2024): 88–94. https://doi.org/10.36320/ajb/v16.i3.17437.

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Since their discovery, diazepines have been essential derivatives that can be found in nature or synthesized in laboratories. We synthesized a new diazepine (4-6), namely 2-[4-(4-chlorophenyl)-2,5-dihydro-1H-1,5-benzodiazepin-2-yl]phenol (4), 2-(4-{2-[(dioxo-l6-sulfanyl)oxy]phenyl}-2,5-dihydro-1H-1,5-benzodiazepin-2-yl)phenol (5), and 2-[4-(2-hydroxyphenyl)-4,5-dihydro-1H-1,5-benzodiazepin-2-yl]benzene-1,3-diol (6). These derivatives are synthesized from 2-hydroxy acetophenone with aldehyde derivatives, such as 4-chlorobenzaldehyde, 2-sulfobenzaldehyde, and 2,6-dihydroxybenzaldehyde. The chalc

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49

Tran, Victor, Craig Forsyth, and Craig Francis. "5-Amino-3-(diethylamino)-5H-benzo[4,5]imidazo[1,2-b][1,2,4,6]thiatriazine 1,1-Dioxide." Molbank 2018, no. 3 (2018): M1018. http://dx.doi.org/10.3390/m1018.

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In the quest for discovery of novel bioactive molecules, new heterocyclic ring systems provide templates for exploration of uncharted chemical space. Herein, we describe the synthesis of a new benzo[4,5]imidazo[1,2-b][1,2,4,6]thiatriazine derivative from readily available 1,2-diaminobenzimidazole and N,N-diethyl-N′-chlorosulfonyl chloroformamidine. The product structure, confirmed by X-ray crystallography, bears an exocyclic NH2 group, which should enable synthesis of an extended range of derivatives of this unusual scaffold.

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50

Kamaike, K., H. Takahashi, K. Morohoshi, N. Kataoka, T. Kakinuma, and Y. Ishido. "Oligonucleotide synthesis using the 2-(levulinyloxymethyl)-5-nitrobenzoyl group for the 5'-position of nucleoside 3'-phosphoramidite derivatives." Acta Biochimica Polonica 45, no. 4 (1998): 949–76. http://dx.doi.org/10.18388/abp.1998_4354.

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A comparative study on the utility of 2-(levulinyloxymethyl)-5-nitrobenzoyl (LMNBz) and 2-(levulinyloxymethyl)benzoyl (LMBz) protecting groups for the 5'-positions of nucleoside 3'-phosphoramidite derivatives in the oligonucleotide synthesis is presented in terms of the syntheses of TpTpT, TpTpTpT, and UpCpApGpUpUpGpG. In addition we describe the synthesis, using the LMNBz protecting group, of the CpCpA terminus triplet of tRNAs bearing exocyclic amino groups with 15N-labeling, and the trimer Gp[A*]pG containing 2'-O-(beta-D-ribofuranosyl)adenosine ([A*]), the latter of which is found at posit

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