A Simple and Efficient New Approach to the Total Synthesis of (±)-4-Amino-3-(4-Chlorophenyl)-Butyric Acid (BACLOFEN)

Abstract

Based on the utilization of a [2+2] cycloaddition reaction between dichloroketene and an appropriated olefin as a key step, we describe a new and simple four step approach to the total synthesis of (±)-4-amino-3-(4-chlorophenyl)-butyric acid (BACLOFEN), a selective GABA_B agonist used as antispastic agent

Notes

For some examples of racemic synthesis of Baclofen and derivatives see: a) Kerberle, H., Faigle, J.W. and Wilhelm, M., Swiss Patent, 499,046, (Chemical Abstracts, 1968, 69, 106273f.