公开(公告)号：US20160060203A1

公开(公告)日：2016-03-03

申请号：US14780625

申请日：2014-03-28

Applicant: KOWA COMPANY, LTD.

Inventor： Yukiyoshi YAMAZAKI

IPC: C07C51/41 ,  C07D263/58 ,  C07C67/08

CPC classification number: C07C51/412 ,  A61K31/423 ,  C07B57/00 ,  C07C67/08 ,  C07D263/58 ,  C07C51/487 ,  C07C59/01

Abstract: To provide a method for improving optical purity of an optically active 2-hydroxycarboxylic acid or a derivative thereof, which is useful as a raw material in the manufacture of medicines, agrochemicais, and industrial products. The method of the invention for improving purity of a hydroxycarboxylic acid of the following formula (1a) or (1b) or a derivative thereof includes the steps of reacting the hydroxycarboxylic acid of the following formula (1a) or (1b) with at least one optically inactive base selected from the group consisting of an alkali metal, alkoxide and a secondary amine in the presence of a solvent and, subsequently, performing recrystallization, to thereby form a hydroxycarboxylic acid salt of the following formula (IIIa) or (IIIb): wherein R1 represents a C1-8 alkyl group, and R2 represents an alkali metal or a secondary amine.

Abstract translation: 提供一种用于提高光学活性的2-羟基羧酸或其衍生物的光学纯度的方法，其可用作制造药物，农用化学品和工业产品中的原料。 本发明提高下式（1a）或（1b）的羟基羧酸的纯度或其衍生物的方法包括以下步骤：使下式（1a）或（1b）的羟基羧酸与至少一种 在溶剂存在下，选自碱金属，醇盐和仲胺的光学非活性碱，然后进行重结晶，从而形成下式（IIIa）或（IIIb）的羟基羧酸盐： 其中R1表示C1-8烷基，R2表示碱金属或仲胺。