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[摘要]:A new method was developed for the synthesis of 6,7-dihydro-5H-pyrimido[4,5-e][1,4]diazepin-8(9H)-one derivatives. The key to construct the pyrimido[4,5-e][1,4]diazepine core is the intramolecular amidation of N-((4-amino-6-chloropyrimidin-5-yl) methyl)-substituted amino acid esters. This methodology was validated through the preparation of 13 representative 6,7-dihydro-5H-pyrimido[4,5-e][1,4]diazepin-8(9H)-ones in moderate to good yields. |
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