Formation of Synthetically Versatile 2-Aminobenzophenones from Readily Accessed Acyl Hydrazides

被引:4
作者
Ahmed, Nehaal [1 ]
Shamsabadi, Andre [1 ]
Chudasama, Vijay [1 ]
机构
[1] UCL, Dept Chem, 20 Gordon St, London WC1H 0AJ, England
基金
英国工程与自然科学研究理事会;
关键词
CATALYZED DIRECT ADDITION; ONE-POT PROCEDURE; POLYSUBSTITUTED QUINOLINES; QUINAZOLINE DERIVATIVES; EFFICIENT SYNTHESIS; FACILE; CONVERSION; ALDEHYDES; ESTERS; ACIDS;
D O I
10.1021/acsomega.9b03417
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Herein, we report the transformation of readily accessed acyl hydrazides into protected 2-aminobenzophenones via a two-step process involving an aryne-based molecular rearrangement followed by a one-pot addition-elimination procedure. The assembly of the scaffold is tolerant of a wide variety of functional groups, and the carbamate group on the product can be facilely removed to afford highly valuable 2-aminobenzophenones. Application of the protocol was demonstrated in the synthesis of neurological medicine phenazepam.
引用
收藏
页码:22601 / 22612
页数:12
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