Simple and Convenient Procedure for the Synthesis of 2 (3 (tert Butoxycarbonylamino)propyl)-5-methylthiophenes

Abstract

Abstract 2-(3-(tert-Butoxycarbonylamino)propyl)-5-methylthiophene and its 4-deuterio derivative have been synthesized by a simple and convenient method in a six step sequence from 2-methylthiophene. The final step involved bromine-lithium exchange on 4-bromo-2-(3-(tert-butoxycarbonylamino)propyl)-5-methylthiophene at low temperature in anhydrous tetrahydrofuran followed by treatment with water or D2O.