Journal of Organic Chemistry p. 1675 - 1681 (1980)
Update date:2022-08-05
Topics:
Gates, Marshall
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 has been 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 has been synthesized.The overall yield is about 50percent from 5-chloroisatoic anhydride.
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Doi:10.1016/S0022-328X(00)83511-1
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(1980)