A Simple and One Step Commercially Cost Effective Process for Eluxadoline Intermediates

K Nageswararao, K Venkateswara

Abstract

Methyl-5-formyl-2-methoxybenzoate (1) and (S)-alpha-Methyl-4-phenyl-1H-imidazole-2-methanamine (2) are key intermediates in the synthesis of Eluxadoline drug. We described a new cost effective process for synthesis of Methyl-5-formyl-2-methoxybenzoate (1) with salicylic acid, Methanesulfonic acid, Hexamethylenetetramine and (S)-alpha-Methyl-4-phenyl-1H-imidazole-2-methanamine (2), with boc-L-Alanine and 2-chloroacetophenone. All the synthetic results were confirmed by ESI-MS and NMR analysis.