发明授权
- 专利标题: Zaleplon synthesis
- 专利标题(中): 扎来普隆合成
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申请号: US10570453申请日: 2004-09-02
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公开(公告)号: US07772394B2公开(公告)日: 2010-08-10
- 发明人: Rajendra Narayanrao Kankan , Dharmaraj Ramachandra Rao
- 申请人: Rajendra Narayanrao Kankan , Dharmaraj Ramachandra Rao
- 申请人地址: IN Mumbai, Maharashtra
- 专利权人: Cipla Limited
- 当前专利权人: Cipla Limited
- 当前专利权人地址: IN Mumbai, Maharashtra
- 代理机构: Conley Rose, P.C.
- 代理商 Rodney B. Carroll
- 优先权: IN913/MUM/2003 20030904
- 国际申请: PCT/GB2004/003757 WO 20040902
- 国际公布: WO2005/023813 WO 20050317
- 主分类号: C07D487/04
- IPC分类号: C07D487/04 ; A61K31/519
摘要:
A process for making zaleplon comprising alkylating 3-[3-(dimethylamino)-1-oxo-2-propenyl]-phenyl]-acetamide with ethyl iodide in the presence of an alkali metal hydroxide or alkoxide selected from sodium hydroxide, potassium hydroxide, sodium methoxide, sodium tert-butoxide or potassium tert-butoxide in an aprotic solvent to give N-ethyl-[3-[3-(dimethylamino)-1-oxo-2-propenyl]-phenyl]-acetamide, condensing N-ethyl-[3-[3-(dimethylamino)-1-oxo-2-propenyl]-phenyl]-acetamide and 3-amino-4-cyanopyrazole, and isolating zaleplon from the reaction. Preferably, the condensing is done in the presence of (a) a water immiscible organic acid; (b) a cation exchange resin; or (c) a water miscible organic acid in water or in a C-1 to C-4 alcohol or in a mixture of water and a C-1 to C-4 alcohol.
公开/授权文献
- US20070191399A1 Zaleplon synthesis 公开/授权日:2007-08-16
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