Invention Grant
- Patent Title: Process for the preparation of alfuzosin hydrochloride
- Patent Title (中): 盐酸阿夫唑嗪的制备方法
-
Application No.: US12671418Application Date: 2008-08-01
-
Publication No.: US08716476B2Publication Date: 2014-05-06
- Inventor: Rajendra Narayanrao Kankan , Dharmaraj Ramachandra Rao , Dilip Birari
- Applicant: Rajendra Narayanrao Kankan , Dharmaraj Ramachandra Rao , Dilip Birari
- Applicant Address: IN Mumbai
- Assignee: Cipla Limited
- Current Assignee: Cipla Limited
- Current Assignee Address: IN Mumbai
- Agency: Conley Rose, P.C.
- Agent Rodney B. Carroll
- Priority: IN1493/MUM/2007 20070802
- International Application: PCT/GB2008/002632 WO 20080801
- International Announcement: WO2009/016387 WO 20090205
- Main IPC: C07D239/95
- IPC: C07D239/95

Abstract:
A process for preparing alfuzosin or a salt thereof comprising: (a) condensing 4-amino-2-chloro-6,7-dimethoxyquinazoline with 3-methylaminopropionitrile in the presence of a polar aprotic solvent selected from the group consisting of diglyme, dimethyl formamide, t-butanol, hexamethylphosphoramide or mixtures thereof to form N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methyl-2-cyanoethylamine (b) hydrogenating the N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methyl-2-cyanoethylamine using a hydrogenating agent under a pressure of less than 10 kg/cm2 to form N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methylpropylenediamine and optionally converting the N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methylpropylenediamine to an acid addition salt thereof; and (c) converting tetrahydrofuroic acid to an intermediate form and condensing the intermediate form with the N-(4-amino-6,7-dimethoxyquinazol-2-yl)-N-methylpropylenediamine or with the acid addition salt to yield alfuzosin base, and optionally converting alfuzosin base to a salt of alfuzosin.
Public/Granted literature
- US20100256370A1 Process for the Preparation of Alfuzosin Hydrochloride Public/Granted day:2010-10-07
Information query