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Parallel Synthesis of Benzofurans

12 February 2015

A series of benzofurans (structures often targeted in diabetes and insulin control research), were synthesized to demonstrate the capabilities of Biotage® Endeavor™ for parallel hydrogenation in drug discovery.

 

Starting out with p-hydroxybenzaldehyde, a four step synthetic pathway led to the synthesis of a benzofuran derivative in high yield and purity using Biotage® Endeavor™ catalyst screening system. With eight parallel reaction chambers, one single run was sufficient to identify optimal catalyst and reaction conditions. The system also handled the final catalytic alkene hydrogenation step while monitoring pressure and temperatures. 

Benzofuran synthesis on Biotage Endeavor

Scheme 1. Synthesis of Benzofuranylmethyl-2,4-Thiazolidinediones.