期刊
JOURNAL OF COMBINATORIAL CHEMISTRY
卷 12, 期 4, 页码 503-509出版社
AMER CHEMICAL SOC
DOI: 10.1021/cc100039w
关键词
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资金
- National Natural Science Foundation of China [90713008]
- National Science & Technology Major Project Key New Drug Creation and Manufacturing Program of China [2009ZX09501-010]
- Changchun Discovery Sciences, Ltd.
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.
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