Title:
PRODUCTION OF CIS COMPOUND OF 2-DIPHENYLMETHYL-N-PHENYLMETHYL-1-AZABICYCLO(2,2,2)OCTAN-3-AMINE COMPOUND
Document Type and Number:
Japanese Patent JP2583026
Kind Code:
B2
Abstract:
PURPOSE: To obtain the subject compound useful as an agent having substance P antagonistic action by reducing an azabicyclo[2,2,2]octan-3-imine compound with sodium triacetoxyborohydride and acetic acid.
CONSTITUTION: The objective racemic cis compound of formula II is produced by reducing a compound of formula I (R1, R2 and R3 are each H, F, Cl, Br, trifluoromethyl, a 1-3C alkyl or a 1-3C alkoxy) with sodium triacetoxyborohydride and acetic acid at 5-50°C. The compound of formula I can be produced from a phenylmethyleneimine intermediate and the racemic mixture of the cis compound of formula II can further be resolved. Substance P is a pharmacologically active neuro-peptide produced by mammals, has a specific amino acid sequence and is useful for the treatment of psychopathy, migraine, rheumatoid arthritis, ulcerative colitis, etc.
Inventors:
GODEKU DENISU EMU
MAATEIASHOO CHAARUZU DABURYUU
MAATEIASHOO CHAARUZU DABURYUU
Application Number:
JP32235394A
Publication Date:
February 19, 1997
Filing Date:
December 26, 1994
Export Citation:
Assignee:
PFIZER
International Classes:
A61K31/435; A61P1/00; A61P25/04; A61P25/06; C07B57/00; C07D453/02; C07D; (IPC1-7): C07D453/02
Attorney, Agent or Firm:
Kyozo Yuasa (5 people outside)
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