发明授权
US08450491B2 Method for the preparation of montelukast acid and sodium salt thereof in amorphous form
有权
用于制备无定形形式的孟鲁司他酸及其钠盐的方法
- 专利标题: Method for the preparation of montelukast acid and sodium salt thereof in amorphous form
- 专利标题(中): 用于制备无定形形式的孟鲁司他酸及其钠盐的方法
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申请号: US10576971申请日: 2003-06-06
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公开(公告)号: US08450491B2公开(公告)日: 2013-05-28
- 发明人: Sanjay Suri , Jujhar Singh , Gurdeep Singh Sarin , Madan Pal Tanwar , Manu Mahendru
- 申请人: Sanjay Suri , Jujhar Singh , Gurdeep Singh Sarin , Madan Pal Tanwar , Manu Mahendru
- 申请人地址: IN New Delhi
- 专利权人: Morepen Laboratories Limited
- 当前专利权人: Morepen Laboratories Limited
- 当前专利权人地址: IN New Delhi
- 代理机构: Reed Smith LLP
- 代理商 Nanda P. B. A. Kumar
- 国际申请: PCT/IN03/00214 WO 20030606
- 国际公布: WO2004/108679 WO 20041216
- 主分类号: C07D215/04
- IPC分类号: C07D215/04 ; A61K31/47
摘要:
A method for the preparation of montelukast acid sodium salt thereof in amorphous form has been described. The method comprises of following steps: (a) generating the dilithium dianion of 1-(mercaptomethyl)cyclopropane acetic acid, by reacting with alkyl lithium, (b) coupling the said dianion with wet mesylate to get montelukast acid in crude form, (c) obtaining DCHA salt in crude form by adding dicyclohexylamine (DCHA) to crude acid obtained in the above step (b), (d) purifying and converting the said DCHA salt in crude form, to montelukast acid in pure form, and (e) reacting the pure montelukast acid in a polar protic solvent with a source of sodium ion followed by evaporating the solvent and triturating of the residue with non-polar water immiscible solvent.