Efficient One-Pot Synthesis of Polyfunctionalized Thiophenes via an Amine-Mediated Ring Opening of EWG-Activated 2-Methylene-1,3-dithioles

An amine-mediated ring-opening reaction of EWG-activated 2-methylene-1,3-dithioles (EWG = electron-withdrawing group) was disclosed,
and a new route to highly substituted thiophenes was developed via the ring opening of 1,3-dithioles and subsequent intramolecular annulation
and amine substitution. This one-pot reaction could proceed efficiently under mild conditions.

本研究报道了吸电子基团（electron-withdrawing group, EWG）活化的2-亚甲基-1,3-二噻环戊烯的胺介导开环反应，并通过1,3-二噻环戊烯开环、后续分子内环化与胺基取代反应，开发了一条制备高取代噻吩类化合物的全新路线。该一锅法反应可在温和条件下高效进行。