A Mild and Inexpensive Procedure for the Synthesis of N,N′-Di-Boc-Protected Guanidines

被引：19
|
作者：
Porcheddu, Andrea [1 ]
De Luca, Lidia [1 ]
Giacomelli, Giampaolo [1 ]
机构：
[1] Univ Sassari, Dipartimento Chim, I-07100 Sassari, Italy
来源：
SYNLETT | 2009年 / 20期
关键词：
cyanuric chloride; TCT; guanidine; N; N '-di-Boc-protected guanidines; guanylating reagent; SOLID-PHASE SYNTHESIS; PROTECTED GUANIDINES; PARALLEL SYNTHESIS; AMINES; REAGENT; GUANYLATION; DERIVATIVES; 1H-PYRAZOLE-1-CARBOXAMIDINE; AMIDINATION; CONVENIENT;
D O I：
10.1055/s-0029-1218365
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A novel and efficient synthetic procedure for converting a diverse set of amines to N,N'-di-Boc-protected guanidines is described. The methodology comprises the use of cyanuric chloride (TCT) as activating reagent for di-Boc-thiourea. The employ of inexpensive TCT instead of classical HgCl2 eliminates the environmental hazard of heavy-metal waste without appreciable loss of yield or reactivity. This protocol provides an alternative route for the guanylation of amines from those currently employed.
引用
收藏
页码：3368 / 3372
页数：5
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