5'-HYDROXY THALIDOMIDE DERIVATIVE AND METHOD FOR PRODUCING THE SAME

摘要

PROBLEM TO BE SOLVED: To provide an optically active 2-(5-hydroxy-2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione derivative which is a thalidomide metabolite and to provide a method for producing the derivative. SOLUTION: The optically active 2-(5-hydroxy-2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione derivative is represented by formula (wherein, R1, R2, R3, R4, R5and R7represent each independently a hydrogen atom, a lower alkyl group, a lower alkoxy group or the like; and R6represents a hydrogen atom or a protecting group of the amino group). The method for production comprises a step of reacting the derivative with an acylating agent in the presence of an enzyme stereoselectively acylating the 5-hydroxy group of the derivative in an organic solvent, forming an optically active ester and thereby carrying out optical resolution. COPYRIGHT: (C)2009,JPO&INPIT