The [4+2] annulation for THIQs.

Abstract

In this research we represented a simple and elegant method for 3,3-disubstituted THIQs via base-mediated [4 + 2] annulation of α-amino acid ester derivatives and 1,2-bis(bromomethyl)benzene under mild conditions. This protocol features good substrate tolerance, mild conditions and moderate to excellent yields. The synthetic potential of this protocol was highlighted by scale-up experiments and further structural elaboration.