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  • Title: Synthesis of novel 8,9-dihydro-5H-pyrimido[4,5-e][1,4]diazepin-7(6H)-ones.
    Author: Xiang J, Wen D, Xie H, Dang Q, Bai X.
    Journal: J Comb Chem; 2010 Jul 12; 12(4):503-9. PubMed ID: 20507170.
    Abstract:
    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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