Synthesis of novel 6,7‐dihydro‐5H‐pyrimido[4,5‐e][1,4]diazepin‐8(9H)‐ones |
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| Authors: | Jinbao Xiang Xiaowei Hu Qun Dang Xu Bai |
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| Institution: | The Center for Combinatorial Chemistry and Drug Discovery, The School of Pharmaceutical Sciences and The College of Chemistry, Jilin University, Changchun, Jilin 130021, People's Republic of China |
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| Abstract: | A new method was developed for the synthesis of 6,7‐dihydro‐5H‐pyrimido4,5‐e]1,4]diazepin‐8(9H)‐one derivatives. The key to construct the pyrimido4,5‐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‐pyrimido4,5‐e]1,4]diazepin‐8(9H)‐ones in moderate to good yields. J. Heterocyclic Chem., (2011). |
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