- Synthesis of ethyl 4-oxo-3,4-dihydro[1]benzofuro[3,2-d]-pyrimidine-2-carboxylate and its derivatives
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The synthesis of ethyl 4-oxo-3,4-dihydro[1]benzofuro[3,2-d]pyrimidine-2-carboxylates was developed to modify the benzofuro-[3,2-d]pyrimidine heterocyclic system.
- Alyabiev, Sergey B.,Kravchenko, Dmitri V.,Ivachtchenko, Alexandre V.
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- ION CHANNEL INHIBITOR COMPOUNDS FOR CANCER TREATMENT
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The present invention concerns a compound of following general formula (I): where: either R is an R1 group and R′ is an -A1-Cy1 group, or R is an -A1-Cy1 group and R′ is an R1 group, R1 particularly being H or (C1-C6)alkyl group;A1 being an —NH— radical or —NH—CH2— radical;Cy1 particularly being a phenyl group,A is a fused (hetero)aromatic ring having 5 to 7 atoms, for use for treating cancer.
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Paragraph 0312; 0313
(2021/01/25)
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- Commercial Copper-Catalyzed Aerobic Oxidative Synthesis of Quinazolinones from 2-Aminobenzamide and Methanol
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The focus of this study was the development of a new synthetic method for quinazolinones based on the principles of Green Chemistry. Quinazolinones were synthesized from 2-aminobenzamide using methanol as both the C1 source and a green solvent in the presence of base Cs2CO3. Additionally, a commercially available, economical copper complex was used as a catalyst in the reaction. The desired products were achieved in moderate to high yield with up to 99 % isolated yield.
- Chatwichien, Jaruwan,Choommongkol, Vachira,Kerdphon, Sutthichat,Meepowpan, Puttinan,Rithchumpon, Puracheth,Sanghong, Patthadon,Singh, Thishana
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supporting information
p. 2730 - 2734
(2020/05/18)
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- SUBSTITUTED TRICYCLIC PYRIDINE OR PYRIMIDINE VANILLOID RECEPTOR LIGANDS
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The present invention relates to substituted tricyclic compounds, which can be used as vanilloid receptor ligands. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by vanilloid receptor-1 (VRl). Also provided herein are pharmaceutical compositions and methods for treating or preventing diseases, conditions and/or disorders modulated by VRl.
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Page/Page column 29
(2009/07/25)
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- Tyrosine kinase inhibitors. 16. 6,5,6-Tricyclic benzothieno[3,2-d]pyrimidines and pyrimido[5,4-b]- and -[4,5- b]indoles as potent inhibitors of the epidermal growth factor receptor tyrosine kinase
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Several elaborations of the fundamental anilinopyrimidine pharmacophore have been reported as potent and selective inhibitors of the epidermal growth factor receptor (EGFr) tyrosine kinase. This paper reports on a series of inhibitors whereby some 6,5-bicyclic heteroaromatic systems were fused through their C-2 and C-3 positions to this anilinopyrimidine pharmacophore. Although the resulting tricycles did not produce the enormous potency of some of the (5/6),6,6-bicyclic systems, the best of them had IC50s for the EGFr TK around 1 nM. Investigation of 4-position side chains in the indolopyrimidines confirmed that m-bromoaniline was an optimal substituent for potency. Investigation of substitution within the C-(benzo)ring of benzothienopyrimidines confirmed that introduction of an extra ring can change sharply the effects of substituents when compared to similar bicyclic nuclei, and only two substituents were found which even moderately enhanced inhibitory activity over the parent compound for this series.
- Showalter, H. D. Hollis,Bridges, Alexander J.,Zhou, Hairong,Sercel, Anthony D.,McMichael, Amy,Fry, David W.
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p. 5464 - 5474
(2007/10/03)
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- Studies in Benzofurans : Part VIII-Synthesis of Some 3-N-aryl-, 3-N-Alkyl- and 3-Amino-3,4-dihydro-4-oxobenzofuropyrimidines
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Ethyl 3-amino-2-benzofuran-carboxylate (I) on condensation with ethyl orthoformate and various aromatic amines affords 3-N-aryl-3,4-dihydro-4-oxobenzofuropyrimidines (II).Analogous 3-alkyl and 3-amino compounds have been prepared by the reaction of ethyl 3-(ethoxymethylene)amino-2-benzofurancarboxylate (III) with aliphatic amines and hydrazine hydrate respectively.
- Mahajan, S. B.,Agasimundin, Y. S.
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p. 402 - 404
(2007/10/02)
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