Cascade Reaction of Tertiary Enaminones, KSCN, and Anilines: Temperature-Controlled Synthesis of 2-Aminothiazoles and 2-Iminothiazoline

By: Yuan, Liu; Liu, Jin; Huang, Kun; Wang, Siyu; Jin, Yi; Lin, Jun

The Journal of organic chemistry

DOI：https://doi.org/10.1021/acs.joc.2c00918

Published：2022-Jul-05

Abstract

A one-pot cascade strategy for the synthesis of 2-aminothiazole derivatives by tertiary enaminones, KSCN, and anilines was developed. By changing the reaction temperature, the three-component reaction could be transformed in different ways to obtain moderate to good yields of polysubstituted 2-aminothiazoles and 2-iminothiazolines. This protocol provides an efficient and concise approach to accessing 2-aminothiazole derivatives with potential bioactivity from readily accessible building blocks and reagents.