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

页码：3368 / 3372

页数：5

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