Sustainable Three‐Component Synthesis of Isothioureas from Isocyanides,Thiosulfonates, and Amines |
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| Authors: | Pieter Mampuys Dr Yanping Zhu Dr Tjøstil Vlaar Dr Eelco Ruijter Prof?Dr Romano V A Orru Prof?Dr Bert U W Maes |
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| Institution: | 1. Organic Synthesis, Department of Chemistry, University of Antwerp, Groenenborgerlaan 171, 2020 Antwerp (Belgium);2. Department of Chemistry and Pharmaceutical Sciences and Amsterdam Institute for Molecules, Medicines and Systems (AIMMS), VU University Amsterdam, De Boelelaan 1083, 1081 HV Amsterdam (The Netherlands) |
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| Abstract: | 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. |
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| Keywords: | copper catalysis isocyanides isothioureas Lewis acids molecular sieves |
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