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Journal articles on the topic 'Pyrido[4'

Author: Grafiati

Published: 7 June 2025

Last updated: 2 August 2025

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1

Refat, Hala M., and Khaled S. Mohamed. "Efficient and convenient synthesis of pyrido [2,1-b]benzothiazole, pyrimidopyrido[2,1-b]benzothiazole and benzothiazolo[3,2-a][1,8]naphthyridine derivatives." Heterocyclic Communications 21, no. 4 (2015): 219–24. http://dx.doi.org/10.1515/hc-2015-0018.

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AbstractNew 3-aryl-pyrido[2,1-b][1,3]benzothiazole derivatives 2a–e were synthesized in excellent yields via the reaction of benzothiazoleacetonitrile (1) with different aromatic aldehydes. The treatment of 2-(benzo[d]thiazol-2-yl)-3-(pyridin-4-yl)acrylonitrile (6) with malononitrile afforded 1-amino-3-(pyridin-4-yl)-3H-pyrido[2,1-b][1,3]benzothiazole-2,4-dicarbonitrile (7), which was allowed to react with a variety of reagents to provide pyrimido[5′,4′:5,6]pyrido[2,1-b][1,3]benzothiazole 8, 9 and [1,3]benzothiazolo[3,2-a][1,8]naphthyridine 10, 15 derivatives. All synthesized products were con

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2

Cablewski, Teresa, Erin J. Carter, Craig L. Francis, Andris J. Liepa, and Michael V. Perkins. "N,N-Dialkyl-N′-Chlorosulfonyl Chloroformamidines in Heterocyclic Synthesis. III. Pyrido- and Pyridazo-Fused [1,2,4,6]Thiatriazine Dioxides." Australian Journal of Chemistry 60, no. 2 (2007): 105. http://dx.doi.org/10.1071/ch06367.

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N,N-Dialkyl-N′-chlorosulfonylchloroformamidines 1 reacted with 2-aminopyridines 2 to give novel pyrido[1,2-b][1,2,4,6]thiatriazine dioxides 3 and pyrido[2,1-c][1,2,4,6]thiatriazine dioxides 4. Reaction of 1 with 3-aminopyridazines 5 afforded pyridazo[3,2-c][1,2,4,6]thiatriazine dioxides 6 and a pyridazo[2,3-b][1,2,4,6]thiatriazine dioxide 7. The compounds 6 and 7 are derivatives of new ring systems.

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3

Koch, Pierre, Dieter Schollmeyer, and Stefan Laufer. "2-(4-Fluorophenyl)-3-(4-pyridyl)pyrido[2,3-b]pyrazine." Acta Crystallographica Section E Structure Reports Online 65, no. 10 (2009): o2512. http://dx.doi.org/10.1107/s1600536809037295.

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4

Koch, Pierre, Dieter Schollmeyer, and Stefan Laufer. "3-(4-Fluorophenyl)-2-(4-pyridyl)pyrido[2,3-b]pyrazine." Acta Crystallographica Section E Structure Reports Online 65, no. 10 (2009): o2546. http://dx.doi.org/10.1107/s1600536809037970.

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5

Deady, L. W., D. Ganame, N. H. Quazi, and S. D. Zanatta. "On The Synthesis of Pyridinylthiobarbituric Acids." Australian Journal of Chemistry 55, no. 4 (2002): 287. http://dx.doi.org/10.1071/ch02050.

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The reaction of N-(pyridin-3-yl) and -4-yl thiourea derivatives with malonyl dichloride in trifluoroacetic acid is shown to be an efficient synthesis of the corresponding thiobarbituric acids. The pyridin-2-yl analogue cleaved and produced, instead, 2-hydroxy-4H-pyrido[1,2a]pyrimidin-4-one.

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6

Yegorova, Tatyana, Bogdan Barnych, and Zoia Voitenko. "Reaction of pyrido[2,1-a]isoindole with 1,4-naphtoquinone and study of the product by spectroscopic methods." French-Ukrainian Journal of Chemistry 4, no. 2 (2016): 33–39. http://dx.doi.org/10.17721/fujcv4i2p33-39.

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Key role of the electronic structure of condensed isoindols in the way of the rearrangement was shown. Influence of the dienophile manifests in the requirement of the cyclic form of the dienophile itself. In the reaction of pyrido[2,1-a]isoindole with naphtoquinone rearrangement product of the first type was obtained and its structure was proven by spectral methods. Spectral criteria for the rearranged adducts of the first type for the pyrido[2,1-a]isoindole in the 13C NMR spectra were established. Products of reactions with naphthoquinone, 4-fluoro-, 2,5-difluorophenylmaleimides were isolated

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7

Andersen, Heidi Gade, David Kvaskoff, and Curt Wentrup. "Bisiminopropadienes R-N=C=C=C=N-R from Pyridopyrimidines." Australian Journal of Chemistry 65, no. 6 (2012): 686. http://dx.doi.org/10.1071/ch12039.

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Chlorination of the N,N′-di(2-pyridyl)malonamide 13a affords 2-chloro-8-methyl-4-(2-(4-picolinyl)imino-4H-pyrido[1,2-a]pyrimidine 17a. Flash vacuum thermolysis of 17a causes efficient ring opening to the valence-tautomeric ketenimine 18a/19a, elimination of HCl, and formation of the bis(4-methyl-2-pyridyl)iminopropadiene, R-N=C=C=C=N-R 20a.

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8

Khan, Muhammad Naeem, Misbahul Ain Khan, Noreen Aslam, Pir Bakhsh Khan, and Ehsan ul Haq. "Tetracyclic Heteroaromatic Systems-Synthesis of Ethoxycarbonylphenylpyrido[3',2':5,6] Thiopyranoquinolines." Pakistan Journal of Scientific & Industrial Research Series A: Physical Sciences 64, no. 3 (2021): 191–94. http://dx.doi.org/10.52763/pjsir.phys.sci.64.3.2021.191.194.

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7-benzylideneamino-5H-thiochromeno[2,3-b]pyridin-5-ones and 9-benzylideneamino-5H-thio- chromeno[2,3-b]pyridin-5-ones, on reaction with ethyl pyruvate to afford 1-ethoxycarbonyl-3-phenyl-12H- pyrido[3',2':5,6]thiopyrano[3,2-f]quinoline-12-ones and 4-ethoxycarbonyl-2-phenyl-7H- pyrido[3',2':5,6]thiopyrano[3,2-h]quinoline-7-ones respectively by the two different methods. These products were precipitated by addition of ethanol, water (1:1), were purified by recrystalizing from appropriate solvents and were characterized from their IR, 1H-NMR, mass spectra and elemental analysis data.

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9

Sun, Yi, Wenfei Huang, Zhiqiang Li, Tao Wang, and Jin Luo. "Design, synthesis, and herbicidal activity of novel 2-(arylamino)-5-methyl-4-methylene-7-(methylthio)-4H-pyrido[4,3-d][1,3]oxazine-8-carbonitrile derivatives." Journal of Chemical Research 43, no. 3-4 (2019): 119–23. http://dx.doi.org/10.1177/1747519819845771.

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A series of 5-methyl-4-methylene-7-methylthio-2-arylmino-4 H-pyrido[4,3- d][1,3]oxazine-8-carbonitrile derivatives were synthesized via tandem aza-Wittig and annulation reactions with { N-[3-acetyl-5-cyano-2-methyl-6-(methylthio)pyridin-4-yl]imino}triphenylphosphorane and aryl isocyanate in dry dichloromethane. Their structures were clearly confirmed by infrared, 1H NMR, 13C NMR, high-resolution mass spectrometry, and X-ray single-crystal diffraction. All newly synthesized compounds were screened for herbicidal activities against monocotyledonous and dicotyledonous plants. The results indicate

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10

Abhishek, S. Saxena, Goel Atul, and Ji Ram Vishnu. "A convenient and expwitious synthesis of annulated N, S-heterocycles." Journal of Indian Chemical Society Vol. 80, Apr 2003 (2003): 311–18. https://doi.org/10.5281/zenodo.5839578.

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Medicinal Chemistry Division, Central Drug Research ln$titute, Lucknow-226 001, India E-mail : vjiram@yahoo.com_ Fax: 91-522-223405 <em>Manuscript received 19 September 2002</em> A convenient synthesis of titiett[2,3-<em>b</em>]pyridines (3), thieno[3,2-<em>c</em>]pxridines (4), pyrazolo[3,4-<em>b</em>]ipyridines (6), thieno[2,3- <em>d</em>]pyrimidines (9), pyridoll,2-althienol2,3-dlpyrimidines (11), pyrido[1,2-<em>a</em>]pyrimido141,51 : 4,5[thien:o[2,3-<em>d</em>]pyrimidines (12), pyrido[1,2-<em>a</em>]pyrimido[4,5-<em>d</em>]pyiimidines (13) and pyrazolor[3,4-<em>d</em>]pyrimido[1,2-a]pyrim

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11

Tiwari, Sangeeta, Ashok K. Yadav, and A. K. Mishra. "Some New Pyrido[2,3-d]pyridimines and their Nucleoside of Biological Importance." E-Journal of Chemistry 7, s1 (2010): S85—S92. http://dx.doi.org/10.1155/2010/812567.

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Chalcones (I) reacted with malanonitrile and ammonium acetate yielded 2-amino-3-cyano-4,6-disubstituted pyridines (II) in excellent yield. 4-Amino-5,7-disubstituted pyrido [2,3-d]pyrimidine-2(1H)-thiones (III), 4-amino-5,7-disubstituted pyrido[2,3-d]pyrimidines (IV) and 4-imino-3,5,7-trisubstituted pyrido[2,3-d]pyrimidin-2(1H)-ones (V) have been synthesized by the condensation of compound (II) with thiourea, formamide and arylisocynate respectively. The ribofuranosidesviz. 4-amino-5,7-disubstituted-1- [2',3',5'-tri-o-benzoyl-β,D-ribofuranosyl]pyrido[2,3-d]pyrimidine-2-(1H)-thiones (VI) and 4-i

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12

Kalyana Sundar, J., S. Natarajan, S. Chitra, et al. "Spectral Analysis and Crystal Structures of 4-(4-Methylphenyl)-6-Phenyl-2,3,3a, 4-Tetrahydro-1H-Pyrido[3,2,1-jk]Carbazole and 4-(4-Methoxyphenyl)-6-Phenyl-2,3,3a, 4-Tetrahydro-1H-Pyrido[3,2,1-jk]Carbazole." ISRN Organic Chemistry 2011 (April 17, 2011): 1–7. http://dx.doi.org/10.5402/2011/541082.

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The crystal structures of 4-(4-methylphenyl)-6-phenyl-2,3,3a,4-tetrahydro-1H-pyrido[3,2,1-jk]carbazole (IIa) and 4-(4-methoxyphenyl)-6-phenyl-2,3,3a,4-tetrahydro-1H-pyrido[3,2,1-jk]carbazole (IIb) were elucidated by single crystal X-ray diffraction. Compound (IIa), C28H25N, crystallizes in the triclinic system, space group P-1, with a=8.936(2) Å,b=10.490(1) Å,c=11.801(1) Å,α=102.69(5)°, β=103.27(3)°,γ=93.80(1)°, and Z=2. The compound (IIb), C28H25NO, crystallizes in the monoclinic system, space group P21/a, with a=11.376(5) Å,b=14.139(3) Å,c=13.237(4) Å,β=97.41(3)°, and Z=4. In both the struct

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13

Tank, Manishkumar Jinabhai, Navinkumar A. Kucha, Chirag G. Naik, Tina R. Barot, and G. M. Malik. "Adamantane-pyrido[2,3-d]pyrimidine Derivatives; Synthesis, Characterization and Investigation of Antimicrobial Study." Oriental Journal Of Chemistry 39, no. 2 (2023): 393–402. http://dx.doi.org/10.13005/ojc/390219.

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Target molecules based on Adamantane-pyrido[2,3-d]pyrimidine derivatives were prepared. Adamantane-pyrido[2,3-d]pyrimidine series using N-(hydroxyadamantan-1-yl)-5-(2,4-substitutedphenyl)-2-Methyl-4-Oxo-7-(2-oxo-2H-Chromen-3-yl)pyrido[2,3-d]Pyrimidine-3(4H)carboxamide (6a-j) was synthesized by reaction between 3-(2-chloroacetyl)-5-(2,4-substitutedphenyl)-2-Methyl-7-(2-Oxo-2H-Chromen-3-yl) pyrido[2,3-d]pyrimidin-4(3H)-one (5a-j) and 3-aminoadamantan-1-ol. These derivatives of Adamantane-pyrido[2,3-d]Pyrimidine were investigated in vitro for their biological characteristics against the strains w

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14

Koreňová, Anna, Alžbeta Krutošíková, Jaroslav Kováč, and Stanislav Celec. "Synthesis and reactions of furo[3,2-c]pyridine derivatives." Collection of Czechoslovak Chemical Communications 52, no. 1 (1987): 192–98. http://dx.doi.org/10.1135/cccc19870192.

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The synthesis of a new type of condensed heterocycle pyrido[3',4':4,5]furo[3,2-b]indole (V) and 1,2,4-triazolo[4'',3'':1',2']pyrido[3',4':4,5]furo[3,2-b]indoles (IX) is described and the substitution nucleophilic reaction with 2-(2-nitrophenyl)-4-chlorofuro[3,2-c]pyridine (X) is presented.

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15

Isakhanyan, A. U., N. Z. Hakobyan, Z. A. Hovasyan, et al. "Synthesis and effect of substituted pyrido[2,3-<i>d</i>]pyrimidine-2,4-diones on <i>In Vitro </i>tumor dna methylation." Журнал общей химии 93, no. 4 (2023): 525–30. http://dx.doi.org/10.31857/s0044460x23040042.

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Reaction of 3-diethylamino-1-aryl-, 3-diethylamino-1-aryl-2-phenyl(4-halophenyl)propane-1-ones hydrochlorides with 6-amino-1,3-dimethyluracil results in heterocyclization products, namely 1,3-dimethyl-7-aryl-5,6dihydro-1 H -pyrido[2,3- d ]pyrimidine-2,4-diones, 1,3-dimethyl-7-aryl-6-phenyl(4-halophenyl)-5,6-dihydro1 H -pyrido[2,3- d ]pyrimidine-2,4-diones and 1,3-dimethyl-7-aryl-6-phenyl-(4-halophenyl)-1 H -pyrido[2,3- d ] pyrimidine-2,4-diones. The effect of the synthesized compounds in vitro tumor DNA methylation was studied.

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16

Koch, Pierre, Dieter Schollmeyer, and Stefan Laufer. "N-{4-[3-(4-Fluorophenyl)pyrido[2,3-b]pyrazin-2-yl]-2-pyridyl}isopropylamine." Acta Crystallographica Section E Structure Reports Online 65, no. 10 (2009): o2557. http://dx.doi.org/10.1107/s1600536809038173.

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17

Yoon, Jeong A., and Young Taek Han. "Efficient Synthesis of Pyrido[3,2-c]coumarins via Silver Nitrate Catalyzed Cycloisomerization and Application to the First Synthesis of Polyneomarline C." Synthesis 51, no. 24 (2019): 4611–18. http://dx.doi.org/10.1055/s-0037-1610730.

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Herein, we report an efficient method for the synthesis of the pyrido[3,2-c]coumarin scaffold, one of the privileged heterocycle-fused coumarin scaffolds, via a AgNO3-catalyzed cycloisomerization of 4-(propynylamino)coumarins obtained from diverse 4-hydroxycoumarins. This concise method affords pyrido[3,2-c]coumarin analogues bearing diverse substituents on the benzene or pyridine ring in moderate to good yields. Moreover, this methodology was extended to the facile synthesis of polyneomarline C, a natural pyrido[3,2-c]coumarin derivative isolated from the Chinese herbal medicine Polyalthia ne

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18

Wolska, Irena, Franciszek Herold, and Marta Maj. "4-(2-Pyridyl)-1H,2H-pyrido[1,2-c]pyrimidine-1,3-dione." Acta Crystallographica Section E Structure Reports Online 59, no. 4 (2003): o511—o513. http://dx.doi.org/10.1107/s1600536803004999.

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19

Bakhite, E. A., A. E. Abdel-Rahman, O. S. Mohamed, and E. A. Thabet. "synthesis of Some New Pyridothienopyrimidines and Related [1,2,4]Triazolopyridothienopyrimidines." Journal of Chemical Research 2003, no. 2 (2003): 58–59. http://dx.doi.org/10.3184/030823403103173156.

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4-Chloro-9-phenyl-7-(2-thienyl)pyrido[3′,2′:4,5]thieno[3,2- d]pyrimidine (5) and 3-amino-3,4-dihydro-4-imino-9-phenyl-7-(2-thienyl)pyrido[3′,2′:4,5]thieno[3,2- d]pyrimidine (19) were prepared and employed as precursors for synthesizing the fused-ring compounds of the title.

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20

Lahmidi, Sanae, El Hassane Anouar, Walid Ettahiri, et al. "Nanoarchitectonics and Molecular Docking of 4-(Dimethylamino)Pyridin-1-Ium 2-3 Methyl-4-Oxo-Pyri-Do[1,2-a]Pyrimidine-3-Carboxylate." Crystals 13, no. 9 (2023): 1333. http://dx.doi.org/10.3390/cryst13091333.

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A retro-Claisen reaction of 1-(4-oxo-4H-pyrido [1,2-a]pyrimidin-3-yl)butane-1,3-dione, 3, in the presence of potassium hydroxide and 4-dimethylamino-pyridine has been carried out, leading to 4-(dimethylamino)pyridin-1-ium 2-methyl-4-oxo-pyrido [1,2-a]pyrimidine-3-carboxylate 5. A plausible mechanism explaining the formation of the title compound has been proposed. A single-crystal X-ray diffraction analysis confirms the crystal structure of the isolated organic salt (5). In the crystal, the title compound adopts a layered structure where there are stacks of cations and anions formed by slipped

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21

Ma, Xingling, Lei Liu, Na Cao, Qiaogen Zou, Kaihe Xiong, and Pingkai Ouyang. "Isolation and Structural Elucidation of Palbociclib’s Eight Process-Related Impurities: Two Identified as New Compounds." Journal of AOAC INTERNATIONAL 99, no. 3 (2016): 638–48. http://dx.doi.org/10.5740/jaoacint.15-0251.

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Abstract Palbociclib is the first U.S. Food and Drug Administration-approved cyclin-dependent kinase inhibitor indicated in combination with letrozole for the treatment of breast cancer. Development of a selective method for the determination of any impurities contained in this drug is significantly important to ensure the quality and safety of palbociclib. In this study, a reliable reversed-phase HPLC method for the separation and determination of eight potential impurities was developed and validated. The structures of two new compounds and six other process-related impurities were character

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22

Veselovská, Lucia, Radek Pohl, Eva Tloušt′ová, et al. "Pyrido-Fused Deazapurine Bases: Synthesis and Glycosylation of 4-Substituted 9H-Pyrido[2′,3′:4,5]- and Pyrido[4′,3′:4,5]pyrrolo[2,3-d]pyrimidines." ACS Omega 5, no. 40 (2020): 26278–86. http://dx.doi.org/10.1021/acsomega.0c04302.

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23

Arbain, D., LT Byrne, MV Sargent, BW Skelton, and AH White. "The Alkaloids of Picrasma javanica: Further Studies." Australian Journal of Chemistry 43, no. 2 (1990): 433. http://dx.doi.org/10.1071/ch9900433.

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The structures of two β- carboline alkaloids previously isolated from Picrasma javanica Bl . ( Simarubaceae ) are revised to 1-ethenyl-4-methoxy-9H-pyrido[3,4-b]indol-8-ol (8-hydroxydehydrocrenatine) (5) and 1-ethyl-4-methoxy-9H-pyrido[3,4-b]indol-8-ol (8-hydroxycrenatine) (6), chiefly on the grounds of a single-crystal X-ray structural determination of the former compound.

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24

Lystsova, Ekaterina A., Alexander S. Novikov, Maksim V. Dmitriev, Andrey N. Maslivets, and Ekaterina E. Khramtsova. "Approach to Pyrido[2,1-b][1,3]benzothiazol-1-ones via In Situ Generation of Acyl(1,3-benzothiazol-2-yl)ketenes by Thermolysis of Pyrrolo[2,1-c][1,4]benzothiazine-1,2,4-triones." Molecules 28, no. 14 (2023): 5495. http://dx.doi.org/10.3390/molecules28145495.

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Acyl(imidoyl)ketenes are highly reactive heterocumulenes that enable diversity-oriented synthesis of various drug-like heterocycles. Such ketenes, bearing heterocyclic substituents, afford angularly fused pyridin-2(1H)-ones in their [4+2]-cyclodimerization reactions. We have utilized this property for the development of a new synthetic approach to pharmaceutically interesting pyrido[2,1-b][1,3]benzothiazol-1-ones via the [4+2]-cyclodimerization of acyl(1,3-benzothiazol-2-yl)ketenes generated in situ. The thermal behaviors of 3-aroylpyrrolo[2,1-c][1,4]benzothiazine-1,2,4-triones and 3-benzoylpy

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25

Arbain, D., and MV Sargent. "The Alkaloids of Picrasma javanica." Australian Journal of Chemistry 40, no. 9 (1987): 1527. http://dx.doi.org/10.1071/ch9871527.

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Extraction of Picrasma javanica B1. (Simarubaceae) has yielded two new P- carboline alkaloids,1-ethenyl-4-methoxy-9 H- pyrido-[3,4-blindol-5-ol (5-hydroxydehydrocrenatine) (4) and l-ethyl-4-methoxy-9H-pyrido[3,4-blindol-5-ol (5-hydroxycrenatine) (5), the structures of which follow from their spectroscopic properties. In addition, the known alkaloids crenatine (2) and dehydrocrenatine (1) were isolated. Attempts to synthesize 1-ethyl-4,5-dimethoxy-9-methyl-9 Hpyrido [3,4-blindole(6) are described.

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26

Wolska, Irena, and Franciszek Herold. "Structural Investigation of Two 4-AryIhexahydro-1H,3H-pyrido[1,2-c]pyrimidine-1,3-diones." Zeitschrift für Naturforschung B 55, no. 11 (2000): 1089–94. http://dx.doi.org/10.1515/znb-2000-1116.

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The X-ray crystal structure determination of 4-(4'-fluorophenyl)hexahydro-1H,3H-pyrido[ 1,2-c]pyrimidine-1,3-dione (5) and 4-(4'-chlorophenyl)hexahydro-1H,3H-pyrido [1,2-c]- pyrimidine-1,3-dione (8) is reported. The crystal structures show the formation of centrosymmetric dimers via intermolecular N-H···O hydrogen bonds. The saturated ring adopts a slightly distorted sofa conformation both in 5 and in 8. In either compound the planar phenyl ring is twisted with respect to the pyrimidine-1,3-dione fragment.

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27

Wang, Cui-ping, Jing-bo Yan, Hai-Jun Chi, Yan Dong, and Zhi-qiang Zhang. "3-(4-Methoxyphenyl)pyrido[2,3-b]pyrazine." Acta Crystallographica Section E Structure Reports Online 66, no. 10 (2010): o2650. http://dx.doi.org/10.1107/s1600536810037943.

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28

Hegab, Mohamed I., Nasser A. Hassan, and Farouk M. E. Abdel-Megeid. "Three-component Reaction of Cycloheptanone, 6-Amino-1,3-Dimethyluracil and Aromatic Aldehydes; X-Ray Structure, and Anti-inflammatory Evaluation of the Products." Zeitschrift für Naturforschung B 63, no. 9 (2008): 1117–26. http://dx.doi.org/10.1515/znb-2008-0917.

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1,3-Dimethyl-5-aryl-1,6,7,8,9,10-hexahydrocyclohepta[5,6]pyrido[2,3-d]pyrimidine-2,4-diones 4a, b (the linear regioisomers) and the Schiff bases, 6-N-benzylidenamino-1,3-dimethyluracil derivatives 5a, b, were isolated from a three-component reaction of cycloheptanone, 6-amino-1,3- dimethyluracil, and 4-chloro- or 4-bromobenzaldehyde. Surprisingly, 1,3-dimethyl-10-aryl-1,5,6,7, 8,9-hexahydrocyclohepta[4,5]pyrido-[2,3-d]pyrimidine-2,4-diones 6f, g (the angular regioisomers which are described for the first time in the literature under the given reaction conditions) and the Schiff bases, 6-N-benz

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29

Sharulatha, Venugopal, Anbazhagan Abinaya, Rajeswari M., and Sundaram Sivakamasundari. "Synthesis, characterization and molecular docking of N-aryl amides of pyrido[1,2-a]pyrimidin2-ones as potential antibacterial agents." Journal of Indian Chemical Society Vol. 97, No. 9b, Sept 2020 (2020): 1584–89. https://doi.org/10.5281/zenodo.5665014.

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Department of Chemistry, Avinashilingam Institute for Home Science and Higher Education for Women, Coimbatore-641 043, Tamil Nadu, India <em>E-mail:</em> abinayachemist@gmail.com <em>Manuscript received online 26 July 2020, accepted 30 August 2020</em> Nitrogen-containing heterocyclic compounds play the most key role in the discovery of new drugs. Among all, pyrimidine possesses a wide spectrum because of its positive pharmacological and biological properties. Some novel amides of pyrido[1,2- <em>a</em>]pyrimidine-2-one acetic acids were synthesized, and the structure of the products was

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30

Koralla, Sravani, and Asha Deepti Choppala. "Novel Pyridopyrimidine-Based Compounds: Design, Synthesis and Cytotoxic Evaluation." Asian Journal of Chemistry 37, no. 7 (2025): 1577–86. https://doi.org/10.14233/ajchem.2025.33671.

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In this study, fifteen novel pyrido[2,3-d]pyrimidine derivatives (11a-o) were successfully designed, synthesized and characterized using spectroscopic techniques. The synthesized compounds were evaluated for their anticancer activity against three human cancer cell lines: MDA-MB-231 (breast cancer), HeLa (cervical cancer) and MCF-7 (breast cancer). The MTT assay results revealed that while some compounds exhibited low to moderate activity, the majority demonstrated potent anticancer effects, with pyrido[2,3-d]pyrimidine derivatives standing out as particularly effective. Among the synthesized

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31

Deau, Emmanuel, Damien Hédou, Elizabeth Chosson, Vincent Levacher, and Thierry Besson. "Convenient one-pot synthesis of N3-substituted pyrido[2,3-d]-, pyrido[3,4-d]-, pyrido[4,3-d]-pyrimidin-4(3H)-ones, and quinazolin-4(3H)-ones analogs." Tetrahedron Letters 54, no. 27 (2013): 3518–21. http://dx.doi.org/10.1016/j.tetlet.2013.04.096.

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32

Haber, H., V. Hagen, and M. Schlender. "Synthese von 6-(pyrid-4-yl)-substituierten Pyrido[: 3-d]pyrimidinen und 1,8-Naphthyridinen." Journal f�r Praktische Chemie 333, no. 4 (1991): 637–42. http://dx.doi.org/10.1002/prac.19913330420.

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33

Wolska, Irena, and Franciszek Herold. "Crystal and Molecular Structure of 4-Arylhexahydro-1H,3H-pyrido[1,2-c]pyrimidine-1,3-dione Derivatives." Zeitschrift für Naturforschung B 57, no. 11 (2002): 1315–19. http://dx.doi.org/10.1515/znb-2002-1118.

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The X-ray crystal structure determination of 4-(2-methylphenyl)hexahydro-1H,3H-pyrido[ 1,2-c]pyrimidine-1,3-dione (2) and 4-(3-methylphenyl)hexahydro-1H,3H-pyrido[1,2-c]- pyrimidine-1,3-dione (3) is reported. The crystal structures show the formation of centrosymmetric dimers via intermolecular N-H···O hydrogen bonds. The saturated ring adopts a slightly distorted halfchair conformation in both 2 and 3. In either compound the planar phenyl ring is twisted with respect to the pyrimidine-1,3-dione fragment.

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34

Dotsenko, Victor V., Elena A. Chigorina, and Sergey G. Krivokolysko. "Synthesis of 7-thia-1,4,6,8-tetraazabenzo[de]anthracenes." Proceedings 9, no. 1 (2018): 31. http://dx.doi.org/10.3390/ecsoc-22-05682.

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New polyheterocyclic ensembles of 8,9,10,11-tetrahydro-7-thia-1,4,6,8-tetraazabenzo[de]anthracenes were prepared by reaction of easily available 5Н-pyrido[2’,3’:2,3]thiopyrano[4,5-b]pyridines with Ас2О or acyl chlorides. The starting 5Н-pyrido[2’,3’:2,3]thiopyrano[4,5-b]pyridines were prepared by reaction of N-methylmorpholinium 4-aryl-3-cyano-6-oxo-1,4,5,6-tetrahydropyridine-2-thiolates with malononitrile dimer.

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35

Bhuyan, Pulak J., Kushal C. Lekhok, and Jagir S. Sandhu. "Studies on Uracils: Synthesis of Tetrazolo[4’,5':1,6]pyrido[2,3-d]pyrimidines by the Action of Cyano Stabilised Carbanions on 6-Azido-5-formyluracils." Journal of Chemical Research 23, no. 3 (1999): 232–33. http://dx.doi.org/10.1177/174751989902300331.

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36

Tang, Chu, Yongju Liang, Shun Bai, et al. "Synthesis and antiproliferative evaluation of novel tetrahydrobenzo[4′,5′]thieno[3′,2′:5,6]pyrido[4,3-d]pyrimidine derivatives." RSC Adv. 4, no. 55 (2014): 29187–92. http://dx.doi.org/10.1039/c4ra03535f.

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37

Youssif, Shaker, Said El-Bahaie, and Esam Nabih. "A Facile One-pot Synthesis of Pyrido[2,3-d]-pyrimidines and Pyrido[2,3-d:6,5-d‘]dipyrimidines." Journal of Chemical Research 23, no. 2 (1999): 112–13. http://dx.doi.org/10.1177/174751989902300223.

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The reactions of enaminones (6-aminouracils) 1a–c and 4 with cyano olefins 2a–b and 5a–f led to the formation of pyrido[2,3- d]pyrimidines. 3a–f and 6a–f in good yield, while the treatment of 4-amino-2-thiouracil 4 with aromatic aldehydes afforded pyridodipyrimidines 7a–c.

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38

Deau, Emmanuel, Damien Hedou, Elizabeth Chosson, Vincent Levacher, and Thierry Besson. "ChemInform Abstract: Convenient One-Pot Synthesis of N3-Substituted Pyrido[2,3-d]-, Pyrido[3,4-d]-, Pyrido[4,3-d]-pyrimidin-4(3H)-ones, and Quinazolin-4(3H)-ones Analogues." ChemInform 44, no. 42 (2013): no. http://dx.doi.org/10.1002/chin.201342163.

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39

Said, Dagdag, Belbahloul Mounir, Anouar Mohamed, Kopp Maria, Anouar Abdellah, and Hmyene Mohamed. "A Facile Three-Steps, One-Pot Synthesis of Novel 2-Alkylamino and 2-Dialkylamino-4H-Pyrido [1, 2-A][1,3,5] Triazin-4-Ones from 2-Aminopyridine and 2-Aminopicolines." International Journal of Current Science Research and Review 05, no. 04 (2022): 976–86. https://doi.org/10.5281/zenodo.6433689.

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Abstract : A straightforward approach to novel 2-dialkylamino-4H-pyrido[1,2-a][1,3,5]triazin-4-ones synthesis is presented. The construction of these compounds was achieved by one-pot synthesis involving condensation of 2-aminopyridine or 2-aminopicolines with ethoxycarbonylisothiocianate, followed by amination of the thioureas, and finally thermal ring closure of resulting guanidines. This allowed access to the unreported title heterocycles. We described an efficient, facile, one-pot synthesis of a novel 2-dialkylamino-4H-pyrido[1,2-a][1,3,5]triazin-4-ones in order to obtain a library of pyri

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40

Toplak, Renata, Jurij Svete, Simona Golič Grdadolnik, and Branko Stanovnik. "Methyl (Z)-2-[(Benzyloxycarbonyl)amino]-3-dimethyl- aminopropenoate in the Synthesis of Heterocyclic Systems. Synthesis of (Benzyloxycarbonyl)amino Substituted Fused Pyrimidinones." Collection of Czechoslovak Chemical Communications 64, no. 2 (1999): 177–89. http://dx.doi.org/10.1135/cccc19990177.

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Methyl (Z)-2-[(benzyloxycarbonyl)amino]-3-dimethylaminopropenoate (1) was used as a reagent for preparation of 3-[(benzyloxycarbonyl)amino] substituted 4H-pyrido[1,2-a]pyrimidin-4-ones 17-21, 4H-pyrimido[1,2-b]pyridazin-4-ones 22 and 23, 5H-[1,2,4]triazolo[2,3-a]- pyrimidin-5-one 24, 5H-thiazolo[3,2-a]pyrimidin-5-one 25, and 4H-pyrazino[1,2-a]pyrimidin-4-one 26. Removal of the benzyloxycarbonyl group by catalytical transfer hydrogenation with Pd/C in the presence of cyclohexene is selective to give 3-amino-4H-pyrido[1,2-a]- pyrimidin-4-ones 27-30 in 85-92% yields, or with hydrogen bromide in a

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41

Aruna Kumari, T., and P. Jayaprasad Rao. "SYNTHESIS OF 2-SUBSTITUTED-4H-PYRIDO[2,3-h]BENZOXAZIN-4-ONES AND 2-SUBSTITUTED PYRIDO[2,3-h]-QUINAZOLIN-4(3H)ONES." Synthetic Communications 32, no. 15 (2002): 2261–67. http://dx.doi.org/10.1081/scc-120005995.

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42

Burova, O. A., N. M. Smirnova, V. I. Pol'shakov, G. S. Chernov, G. A. Losev, and T. S. Safonova. "Pyrido[2,3-d]pyrimidines 4. Synthesis and some transformations of oxo(hydroxy)pyrido[2,3-d]pyrimidines." Chemistry of Heterocyclic Compounds 27, no. 5 (1991): 538–44. http://dx.doi.org/10.1007/bf00474003.

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43

Bhaskar, J. Udaya, G. Srinivasa Rao, Pranab Chatterjee, D. K. Sahoo, S. Srinivasa Rao, and B. Pulla Rao. "Synthesis, Characterization and Antibacterial Activity of Some Novel Pyrido[2,3-b]indole, Morpholine and Chalcone Hybrid Compounds." Asian Journal of Chemistry 36, no. 11 (2024): 2598–602. http://dx.doi.org/10.14233/ajchem.2024.32585.

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In present investigation, a novel series of (E)-3-(2-morpholino-9H-pyrido[2,3-b]indol-3-yl)-1-phenylprop-2-en-1-one and its derivatives (5a-f) were synthesized by condensation reaction from the final intermediate, 2-morpholino-9H-pyrido[2,3-b]indol-3-carbaldehyde (4). The synthesis of the title compounds commenced from commercially available 21H-indol-2-amine (1) and by involving N-(1H-indol-2-yl)-acetamide (2) and 2-chloro-9H-pyrido[2,3-b]indole-3-carbaldehyde (3) as reactive intermediates. The chemical structure of synthesized compounds was characterized by IR, 1H NMR, mass spectral data and

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44

Dawande, Sudam Ganpat, Bapurao Sudam Lad, Sunitkumar Prajapati, and Sreenivas Katukojvala. "Rhodium-catalyzed pyridannulation of indoles with diazoenals: a direct approach to pyrido[1,2-a]indoles." Organic & Biomolecular Chemistry 14, no. 24 (2016): 5569–73. http://dx.doi.org/10.1039/c6ob00360e.

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45

Graf, Franziska, Lena Koehler, Torsten Kniess, Frank Wuest, Birgit Mosch, and Jens Pietzsch. "Cell Cycle Regulating Kinase Cdk4 as a Potential Target for Tumor Cell Treatment and Tumor Imaging." Journal of Oncology 2009 (2009): 1–12. http://dx.doi.org/10.1155/2009/106378.

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The cyclin-dependent kinase (Cdk)-cyclin D/retinoblastoma (pRb)/E2F cascade, which controls the G1/S transition of cell cycle, has been found to be altered in many neoplasias. Inhibition of this pathway by using, for example, selective Cdk4 inhibitors has been suggested to be a promising approach for cancer therapy. We hypothesized that appropriately radiolabeled Cdk4 inhibitors are suitable probes for tumor imaging and may be helpful studying cell proliferation processes in vivo by positron emission tomography. Herein, we report the synthesis and biological, biochemical, and radiopharmacologi

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46

Gomha, Sobhi, Ikhlass Abbas, Mohamed Elneairy, Mahmoud Elaasser, and Bazada Mabrouk. "Antimicrobial and anticancer evaluation of a novel synthetic tetracyclic system obtained by Dimroth rearrangement." Journal of the Serbian Chemical Society 80, no. 10 (2015): 1251–64. http://dx.doi.org/10.2298/jsc141222022g.

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A series of pyrido[3',2':4,5]thieno[2,3-e][1,2,4]triazolo[4,3-c]pyrimidines were prepared via oxidative cyclization of 4-(2-arylidenehydrazinyl)pyrido [3',2':4,5]thieno[3,2-d] pyrimidines. Dimroth rearrangement of such a series yielded pyrido[3',2':4,5]thieno[2,3-e][1,2,4]triazolo[1,5-c]pyrimidines. The reaction mechanism was proposed and the products were screened for their antimicrobial and anticancer activities. From the antimicrobial screening results, it can be seen that compounds 8c, 9f and 10c showed excellent activity against gram positive bacteria while compounds 10d and 8c showed the

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47

Xie, Ying, Tengfei Chen, Shaomin Fu, Huanfeng Jiang, and Wei Zeng. "Pd-catalyzed carbonylative cycloamidation of ketoimines for the synthesis of pyrido[1,2-a]pyrimidin-4-ones." Chemical Communications 51, no. 45 (2015): 9377–80. http://dx.doi.org/10.1039/c5cc02631h.

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48

Rashid, Muhammad, Muhammad Khalid, Abida Ashraf, et al. "Multicomponent synthesis of pyrido[2,3-b]pyrazine derivatives: electrochemical DNA sensing, nonlinear optical properties and biological activity." RSC Advances 13, no. 46 (2023): 32160–74. http://dx.doi.org/10.1039/d3ra05365b.

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49

de Meester, P., S. S. C. Chu, M. V. Jovanovic, and E. R. Biehl. "10-(4-Methoxyphenyl)pyrido[3,2-b][1,4]benzothiazine, C18H14N2OS." Acta Crystallographica Section C Crystal Structure Communications 41, no. 8 (1985): 1246–49. http://dx.doi.org/10.1107/s0108270185007302.

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50

Vasil’ev, L. S., S. V. Baranin, A. V. Ignatenko, Yu V. Nelyubina, and V. A. Dorokhov. "Synthesis of 4-(trifluoromethyl)pyrido[4,3-d]pyrimidine derivatives." Russian Chemical Bulletin 59, no. 7 (2010): 1403–7. http://dx.doi.org/10.1007/s11172-010-0254-5.

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