Calcium bis [ (2S) - 3- [3-[ (2S) -3- (4-chloro-2-cyanophenoxy) -2- fluoropropoxy]phenyl ]-2-isopropoxypropionate] and intermediate thereof
申请人:Shinoda Masanobu
公开号:US20070117866A1
公开(公告)日:2007-05-24
The present invention relates to calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate] represented by formula (I), a hydrate thereof, a crystal of the compound of formula (I), and a crystal of the hydrate of the compound of formula (I) which are useful as pharmaceuticals, and to processes for producing the same, and intermediates therefore, and processes for production thereof. [Problem]There is need for (2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, in the form of a drug substance, purified so as to minimize a residual solvent content and having a uniformized specification and a highly favorable workability, and a process for producing the same. [Solution]Crystalline calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate], a calcium salt of (2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, solves the above problem. [Selected Drawing] None
本发明涉及由式(I)表示的双[(2S)-3-[3-[(2S)-3-(4-氯-2-氰基苯氧基)-2-氟丙氧基]苯基]-2-异丙氧基丙酸钙水合物,该水合物的晶体以及作为药物有用的式(I)化合物的晶体,以及其制备方法和中间体,以及生产过程。【问题】需要以药物物质的形式纯化(2S)-3-[3-[(2S)-3-(4-氯-2-氰基苯氧基)-2-氟丙氧基]苯基]-2-异丙氧基丙酸,以使残留溶剂含量最小化,并具有统一的规格和高度有利的可操作性,以及制备该药物物质的方法。【解决方案】结晶的双[(2S)-3-[3-[(2S)-3-(4-氯-2-氰基苯氧基)-2-氟丙氧基]苯基]-2-异丙氧基丙酸钙,即(2S)-3-[3-[(2S)-3-(4-氯-2-氰基苯氧基)-2-氟丙氧基]苯基]-2-异丙氧基丙酸的钙盐,解决了上述问题。【选定图纸】无