NEW SYNTHESIS OF DIAZEPAM

NEW SYNTHESIS OF DIAZEPAM
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DOI:
10.1021/jo01297a030
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发表时间:
1980-01-01
影响因子:
3.6
通讯作者:
GATES, M
GATES, M
中科院分区:
化学2区
文献类型:
--
作者:
GATES, M

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An efficient preparation of 7-chloro-1-methyl-3,4-dihydro-1H-1,4-benzodiazepine-2,5-dione from 5-chloro-N-methylisatoic anhydride and glycine was devised, and from it, by the action of phenylmagnesium chloride on its N-acetyl derivative followed by treatment with hydroxylamine and cleavage of the resulting desacetyl oxime with sodium bisulfite, diazepam was synthesized. The overall yield is .apprx. 50% from 5-chloroisatoic anhydride.