Aminothiolation of alkenes with azoles and Bunte salts
Bingqing Ouyang- 1The Second Norman Bethune Hospital of Jilin University, China
- 2Outpatient Department, The Second Norman Bethune Hospital of Jilin University, China
- 3Department of Pharmacy, Second Affiliated Hospital of Jilin University, China
We have developed an intermolecular aminothiolation of simple olefins using Bunte salt as a thiolating agent. This protocol produces thiyl free radicals under PIDA oxidation conditions, eliminating the need for transition-metal catalysts. The method has a wide range of substrate applicability and is suitable for large-scale preparation and late-stage modification of drug molecules.The simultaneous introduction of sulfur and nitrogen moieties into small molecules is a classical approach for designing new drugs. β-Amino sulfide is an important and widely present scaffold in natural products, bestselling drugs, and small molecular catalysts (Scheme 1A) (Cecchetti et al., 2003;Hosseini-Zare et al., 2011).For a long time, synthetic chemists have devoted considerable effort to develop novel and efficient strategies for the preparation of these significant frameworks (De
Keywords: aminothiolation, Bunte salts, Alkenes, Metal-free, multi-component cascade reactions
Received: 26 Oct 2023;
Accepted: 02 Nov 2023.
Copyright: © 2023 Ouyang, Chai, Li, Zhang and Liu. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
* Correspondence: Mx. Xingmei Liu, Department of Pharmacy, Second Affiliated Hospital of Jilin University, Changchun, Hebei Province, China