An improved synthesis of N-Boc protected aryl amines

被引:53
作者
Darnbrough, S [1 ]
Mervic, M [1 ]
Condon, SM [1 ]
Burns, CJ [1 ]
机构
[1] Aventis Pharmaceut, Dept Med Chem, Collegeville, PA 19426 USA
关键词
D O I
10.1081/SCC-100106036
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
There are several known methods of protecting amines as their Boc derivatives. For less nucleophilic amines such as aryl amines these methods often give poor yields and are generally not satisfactory. Here, Boc aryl amines are obtained by first introducing two Boc groups followed by selective removal of one of them. This procedure works well for a number highly sterically hindered substrates as well as electron deficient and electron rich aryl amines.
引用
收藏
页码:3273 / 3280
页数:8
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