Title:
PRODUCTION OF PAROXETINE
Document Type and Number:
Japanese Patent JP3882224
Kind Code:
B2
Abstract:
PROBLEM TO BE SOLVED: To efficiently obtain the subject compound useful as a medicine by reacting an N-alkylpiperidine compound with a halogenated formic acid ester and subsequently hydrolyzing the obtained alkoxycarbonylpiperidine compound under an alkaline condition.
SOLUTION: (A) An N-alkylpiperidine compound of formula I (R1 is a lower alkyl, a cyclic lower alkyl, an aralkyl, etc.; X is a halogen) is reacted with (B) a halogenated formic acid ester of formula II (R2 is a lower alkyl, a cyclic lower alkyl, an aralkyl, etc.) preferably in the presence of a base to obtain (C) an alkoxycarbonylpiperidine compound of formula III. The component C is subsequently hydrolyzed under an alkaline condition to obtain (D) paroxetine of formula IV. The reaction temperature of the reaction is preferably 10-150°C. The component B is preferably used in an amount of the same or more equivalent as that of the component A, most preferably 1-10 fold equivalents.
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Inventors:
King bell
Yasushi Matsumura
Yasushi Matsumura
Application Number:
JP13904896A
Publication Date:
February 14, 2007
Filing Date:
May 31, 1996
Export Citation:
Assignee:
Asahi Glass Co., Ltd.
International Classes:
C07D405/12; A61K31/443; A61K31/445; A61P25/00; A61P25/24; A61P25/26; A61P43/00; (IPC1-7): C07D405/12; //A61K31/445; A61K31/445; A61K31/445; C07M7:00
Domestic Patent References:
| JP62129280A | ||||
| JP58174363A | ||||
| JP7258196A | ||||
| JP61180769A | ||||
| JP6312988A | ||||
| JP3502696A |
Foreign References:
| WO1995017439A1 |
Attorney, Agent or Firm:
Yoko Hasegawa
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