Sustainable Three‐Component Synthesis of Isothioureas from Isocyanides, Thiosulfonates, and Amines1. Issue 47 (15th September 2014)

• Record Type: Journal Article
• Authors: Mampuys, Pieter; Zhu, Yanping; Vlaar, Tjøstil; Ruijter, Eelco; Orru, Romano V. A.; Maes, Bert U. W.
• Is Part Of: Angewandte Chemie international edition. Volume 53:Issue 47(2014)
• Page Start: 12849
• Page End: 12854
• Publication Date: 2014-09-15
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1002/anie.201406717
• Languages: English
• ISSNs: 1433-7851

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>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 <italic>S</italic>‐alkyl and <italic>S</italic>‐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.</p> </abstract>