A new reagent for solid and solution phase synthesis of protected guanidines from amines

被引:49
作者
Yong, YF [1 ]
Kowalski, JA [1 ]
Thoen, JC [1 ]
Lipton, MA [1 ]
机构
[1] Purdue Univ, Dept Chem, W Lafayette, IN 47907 USA
关键词
D O I
10.1016/S0040-4039(98)80017-8
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A new reagent -4-nitro-1-H-pyrazole-1-[N, N'-bis(tert-butoxycarbonyl)]carboxamidine - has been developed to effect the rapid and efficient synthesis of bis(carbamate)-protected guanidines from primary and secondary amines. The reagent is a more electrophilic, and consequently more reactive, derivative of the literature reagent 1-H-pyrazole-1-[N, N'-bis(tert-butoxycarbonyl)]carboxamidine The increased reactivity of the new reagent affords it increased yields in solution and the need for fewer equivalents when guanylating resin-bound amines. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:53 / 56
页数:4
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