Santhosh Kumar Gautham, Jitender Dev Gaddameedi, Ravi Kumar Nagiri, Krishna Swaroop Desireddy, Poorna Chandra Yedla, Ganesh Kumar Chityala, Narsaiah Banda
Fluoroorganic Division, Indian Institute of Chemical Technology.
Chem Pharm Bull (Tokyo). 2015;63(8):584-90. doi: 10.1248/cpb.c15-00219.
A series of novel pyrido[1,2-a]pyrimidine-3-carboxamide derivatives 6a-n were prepared starting from 2(1H) pyridone 1 via hydrolysis, de-carboxylation, selective O-alkylation followed by rearrangement to give pyridine-2-amine 3. Compound 3 on reaction with ethoxy methylene malonic diethyl ester (EMME) under a conventional method followed by cyclization under micro wave irradiation (MWI) conditions resulted in product 5. Compound 5 on coupling with diverse substituted aliphatic amines formed title compounds 6a-n. All the products 6a-n were screened against four human cancer cell lines and compounds 6h-k and n which showed promising anticancer activity have been identified.
从2(1H)吡啶酮1开始，通过水解、脱羧、选择性O-烷基化，然后重排得到吡啶-2-胺3，制备了一系列新型吡啶并[1,2-a]嘧啶-3-甲酰胺衍生物6a-n。化合物3在常规方法下与乙氧基亚甲基丙二酸二乙酯(EMME)反应，然后在微波辐射(MWI)条件下环化，得到产物5。化合物5与各种取代脂肪胺偶联形成标题化合物6a-n。对所有产物6a-n针对四种人类癌细胞系进行了筛选，已鉴定出显示出有前景的抗癌活性的化合物6h-k和n。
