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Title:
IMPROVED SYNTHESIS OF 1-PIPERIDINYL-1,4-BENZODIAZEPINE
Document Type and Number:
Japanese Patent JPS6038380
Kind Code:
A
Abstract:

PURPOSE: To obtain the titled compound useful as a psychotropic agent such as an antidepressant, antianxiety agent, anticonvulsant, etc. by a short process in high yield, by reacting an aminobenzophenonimine derivative with a glycine ester, treating the reaction product with an acid.

CONSTITUTION: A compound shown by the formula I (R is H, or alkyl; X and Y are H, or halogen) is reacted with a glycine ester (preferably used as a salt of mineral acid such as hydrochloride, etc.) in a solvent such as methanol, etc. at about the boiling point of the solvent under heating, to give a compound shown by the formula II. The compound is then subjected to ring closure with an acid such as trifluoroacetic acid, methanesulfonic acid, etc. at 20W150°C, preferably at 50W100°C, to give the desired substance shown by the formula III.


Inventors:
ADACHI MAKOTO
SAKURA KAZUYUKI
SUGASAWA TSUTOMU
Application Number:
JP14786083A
Publication Date:
February 27, 1985
Filing Date:
August 11, 1983
Export Citation:
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Assignee:
SHIONOGI SEIYAKU KK
International Classes:
C07D207/14; C07D211/58; C07D243/28; C07D401/04; C07D403/04; (IPC1-7): C07D211/58; C07D401/04
Domestic Patent References:
JP43014689A
JPS47814A
Attorney, Agent or Firm:
Mitsutaka Iwasaki