Practical synthesis of KRP203: An unusual styrene coupling reaction

ORGN 70

Masao Chino, chino.masao@ma.m-pharma.co.jp, pharmaceuticals research devision, Mitsubishi Pharma Corporation, 1000 kamoshida-cho, aoba-ku, yokohama, 227-0033, Japan
A practical synthesis of the S1P1 agonist, KRP203 is described. As a key reaction, an unusual coupling of styrene with malonate gives KRP203 core structure. Gram quantities of the targeted drug KRP203 for several biological researches were obtained via six steps in 70% overall yield.