发明授权
US07446227B2 Process for preparation of 5H-dibenzo[a,d] cycloheptene derivatives
有权
制备5H-二苯并[a,d]环庚烯衍生物的方法
- 专利标题: Process for preparation of 5H-dibenzo[a,d] cycloheptene derivatives
- 专利标题(中): 制备5H-二苯并[a,d]环庚烯衍生物的方法
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申请号: US11609075申请日: 2006-12-11
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公开(公告)号: US07446227B2公开(公告)日: 2008-11-04
- 发明人: Satyam Nampalli , Brijesh Patel , Peter Xavier Tharial , Ravishanker Kovi
- 申请人: Satyam Nampalli , Brijesh Patel , Peter Xavier Tharial , Ravishanker Kovi
- 申请人地址: US NJ Somerset
- 专利权人: Apicore, LLC
- 当前专利权人: Apicore, LLC
- 当前专利权人地址: US NJ Somerset
- 代理机构: Kaplan Gilman Gibson & Dernier LLP
- 代理商 Timothy X. Gibson
- 主分类号: C07C211/00
- IPC分类号: C07C211/00
摘要:
A process for preparation of protriptyline hydrochloride from 5-dihydrobenzocycloheptatriene of formula (1) by coupling with chloropropyl alcohol in the presence of excess n-butyl Lithium in tetrahydrofuran under inert atmosphere, followed by preparation of mesylate derivative of formula (3) and finally the nucleophilic displacement of the mesylate group by reacting methylamine solution in methanol to give protriptyline free base of the formula (4). Also the present process reveals the hydrochloride salt formation and purification of the same to give pure pharmaceutical grade protriptyline hydrochloride with impurities less than 0.1% w/w.
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