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Sustainable Three‐Component Synthesis of Isothioureas from Isocyanides, Thiosulfonates, and Amines
Author(s) -
Mampuys Pieter,
Zhu Yanping,
Vlaar Tjøstil,
Ruijter Eelco,
Orru Romano V. A.,
Maes Bert U. W.
Publication year - 2014
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.201406717
Subject(s) - chemistry , aryl , formal synthesis , alkyl , component (thermodynamics) , combinatorial chemistry , organic chemistry , physics , thermodynamics
Multiple applications of isothioureas as fine chemicals (or their precursors) are known, but a general sustainable method for their synthesis was hitherto unavailable. We report a novel general approach towards S ‐alkyl and S ‐aryl isothioureas through a copper(I)‐catalyzed three‐component reaction between amines, isocyanides, and thiosulfonates. The formal synthesis of a superpotent sweetener further illustrates the applicability of our method.