Title:
OPTICAL RESOLUTION OF SUBSTITUTED PIPERIDINE
Document Type and Number:
Japanese Patent JP2549609
Kind Code:
B2
Abstract:
PURPOSE: To efficiently resolve a racemic mixture of cis-3-(2- methoxybenzylamino)-2-phenylpiperidine in an organic solvent such as isopropanol using (R)-(-) mandelic acid as a resolving agent.
CONSTITUTION: A racemic mixture of cis-3-(2-methoxybenzylamino)-2- phenylpiperidine is optically resolved to obtain (+)-cis-3-(2- methoxybenzylamino)-2-phenylpiperidine. The reaction is carried out using (R)-(-) mandelic acid as an optical resolving agent and methanol, ethanol or isopropanol (isopropanol is preferable among them) as a reaction inert organic solvent, then the solvent is removed by filtration and the salt obtained is treated with a base (NaOH is suitable in particular) to give (+) isomer. The thus prepared substituted piperidines and related substances are substance P receptor antagonists and therefore useful for the treatment of diseases mediated by an excess of substance P.
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Inventors:
DENISU EMU GOODETSUKU
TERII JEI ROOZUN
TERII JEI ROOZUN
Application Number:
JP32230594A
Publication Date:
October 30, 1996
Filing Date:
December 26, 1994
Export Citation:
Assignee:
PFIZER
International Classes:
C07B53/00; C07B57/00; C07D211/26; C07D211/56; C07D213/54; C07D213/73; C07D213/74; C07D213/75; C07D401/12; C07D405/12; C07D409/04; C07D409/12; C07D409/14; C07D; (IPC1-7): C07D211/56; C07B57/00
Attorney, Agent or Firm:
Yoshio Kawaguchi (2 outside)