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■ Efficient One-Pot, Three-Step Synthesis of 1,2,3,5-Tetrasubstituted Pyrroles via Aza-Michael Addition of Methyl 3-Iminoacrylates

Michiyasu Nakao,* Ken Horikoshi, Syuji Kitaike, and Shigeki Sano*

*Graduate School of Pharmaceutical Sciences, Tokushima University, 1-78 Sho-machi, Tokushima 770-8505, Japan

Abstract

An efficient one-pot, three-step procedure for the aza-Michael addition of methyl 3-iminoacrylates with secondary amines followed by intramolecular cyclization and silylation successfully afforded novel 1,2,3,5-tetrasubstituted pyrroles in high yields.