发明申请
US20080139848A1 PROCESS FOR PREPARATION OF 5H-DIBENZO[A,D] CYCLOHEPTENE DERIVATIVES
有权
制备5H-二苯并[A,D]环己基衍生物的方法
- 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]环己基衍生物的方法
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申请号: US11609075申请日: 2006-12-11
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公开(公告)号: US20080139848A1公开(公告)日: 2008-06-12
- 发明人: Satyam S. Nampalli , Brijesh Patel , Peter Xavier Tharial , Ravishanker Kovi
- 申请人: Satyam S. 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
- 主分类号: C07C33/16
- IPC分类号: C07C33/16 ; C07C211/31
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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