Synthesis of Novel 8,9-Dihydro-5H-pyrimido[4,5-e][1,4]diazepin-7(6H)-ones

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• 作者：Jinbao Xiang ; Dongsheng Wen ; Hongxiang Xie ; Qun Dang ; Xu Bai
• 刊名：Journal of Combinatorial Chemistry
• 出版年：2010
• 出版时间：July 12, 2010
• 年：2010
• 卷：12
• 期：4
• 页码：503-509
• 全文大小：154K
• 年卷期：v.12,no.4(July 12, 2010)
• ISSN：1520-4774

文摘

Practical and efficient methods have been developed for the synthesis of 4,6,8,9-tetrasubstituted 8,9-dihydro-5H-pyrimido[4,5-e][1,4]diazepin-7(6H)-ones from 4,6-dicholoropyrimidine aldehyde, N-substituted amino acid esters, and amines in five steps. This synthetic strategy is based on suitably substituted pyrimidines as bis-electrophilic species reacting with various amines to construct the pyrimido[4,5-e][1,4]diazepine core with a strategically anchored functional group for further derivatization. The utility of this methodology was demonstrated through the preparation of a 33-membered library of representative 8,9-dihydro-5H-pyrimido[4,5-e][1,4]diazepin-7(6H)-ones in good to excellent yields.