A One-Pot Assembly of Fully Substituted Alkyl 5-Aminothiophene-2-carboxylates from Allenes, Isothiocyanates, and Alkyl 2-Bromoacetates

J Org Chem. 2017 Jul 21;82(14):7519-7528. doi: 10.1021/acs.joc.7b01217. Epub 2017 Jul 5.

Abstract

A novel simple approach to highly functionalized multisubstituted thiophenes such as alkyl 4-alkoxy-5-amino-3-methylthiophene-2-carboxylates through the one-pot sequential reaction of α-lithiated alkoxyallenes with isothiocyanates and alkyl 2-bromoacetates has been discovered. The process proceeds quickly (30-45 min) via in situ formation and intramolecular cyclization of alkyl 2-[(2-alkoxybuta-2,3-dienimidoyl)sulfanyl]acetates (1-aza-1,3,4-trienes).

Publication types

  • Research Support, Non-U.S. Gov't