A simple solid-phase synthesis of disubstituted guanidines using Rink amide resin as an amine component

被引:22
作者
Li, M [1 ]
Wilson, LJ [1 ]
Portlock, DE [1 ]
机构
[1] Procter & Gamble Pharmaceut, Hlth Care Res Ctr, Mason, OH 45040 USA
关键词
disubstituted guanidines; solid-phase synthesis; Rink amide resin;
D O I
10.1016/S0040-4039(01)00162-9
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A practical solid-phase synthesis that simply uses Rink amide resin as an amine component in reacting with aromatic isothiocyanates and aliphatic amines to generate disubstituted guanidines is described. No special linker or guanylation reagents are involved in this method. The product is obtained in a 'traceless-linker' fashion and in high yield and purity when an electron-deficient isothiocyanate is employed. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2273 / 2275
页数:3
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