New route to preparation of loxoprofen through Mizoroki-Heck reaction as the key step

Abstract

The current study describes a new preparation of loxoprofen. The whole process includes five steps from cheap cyclopentanone and methyl 4-bromophenylacetate as the starting materials. The key ­intermediate is obtained through Mizoroki-Heck reaction of 2-methylenecyclopentanone and methyl 2-(4-bromophenyl)propanoate. The desired loxoprofen is yielded through hydrogenation followed by hydrolysis in 56% overall yield with 99.7% purity.