Chemo‐Enzymatic Synthesis of Navarixin by Using Aqueous Micellar Media: A Greener Approach

Abstract

AbstractA mild and scalable chemo‐enzymatic procedure for the synthesis of the anticancer drug navarixin was developed in aqueous micellar media. We herein, report a greener methodology for the synthesis of a key chiral amine intermediate in the synthesis of navarixin using transaminases. This was obtained in high yields with an enantiomeric excess of >99.9 %. The current synthetic method represents a mild and sustainable procedure to afford the chiral amine intermediate in a single step without the use of expensive chiral ligands and auxiliaries. Furthermore, the chiral amine was used in the synthesis of navarixin which was obtained in high yield and an enantiomeric excess of >97.7 %.