对三氟乙酸敏感的芳基磺酰基硫脲辅助合成N,N'-取代胍。

TFA-sensitive arylsulfonylthiourea-assisted synthesis of N,N'-substituted guanidines.

作者信息

Li Jizhen, Zhang Guangtao, Zhang Zhongsheng, Fan Erkang

机构信息

Biomolecular Structure Center, Department of Biochemistry, University of Washington, Seattle, Washington 98195, USA.

出版信息

J Org Chem. 2003 Feb 21;68(4):1611-4. doi: 10.1021/jo026807m.

DOI:10.1021/jo026807m

PMID:12585918

Abstract

An efficient synthesis of N,N'-substituted guanidine derivatives was developed via an aromatic sulfonyl-activated thiourea intermediate. The use of certain aromatic sulfonamides, such as PbfNH(2), as the key reagent to incorporate a TFA-labile guanidine protection group greatly facilitates solid-phase synthesis of N,N'-substituted guanidine compounds.

摘要

通过芳基磺酰基活化的硫脲中间体开发了一种高效合成N，N'-取代胍衍生物的方法。使用某些芳基磺酰胺，如PbfNH(2)，作为引入对三氟乙酸不稳定的胍保护基的关键试剂，极大地促进了N，N'-取代胍化合物的固相合成。