Invention Grant
- Patent Title: Zaleplon synthesis
- Patent Title (中): 扎来普隆合成
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Application No.: US10570453Application Date: 2004-09-02
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Publication No.: US07772394B2Publication Date: 2010-08-10
- Inventor: Rajendra Narayanrao Kankan , Dharmaraj Ramachandra Rao
- Applicant: Rajendra Narayanrao Kankan , Dharmaraj Ramachandra Rao
- Applicant Address: IN Mumbai, Maharashtra
- Assignee: Cipla Limited
- Current Assignee: Cipla Limited
- Current Assignee Address: IN Mumbai, Maharashtra
- Agency: Conley Rose, P.C.
- Agent Rodney B. Carroll
- Priority: IN913/MUM/2003 20030904
- International Application: PCT/GB2004/003757 WO 20040902
- International Announcement: WO2005/023813 WO 20050317
- Main IPC: C07D487/04
- IPC: C07D487/04 ; A61K31/519

Abstract:
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.
Public/Granted literature
- US20070191399A1 Zaleplon synthesis Public/Granted day:2007-08-16
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