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Title:
3-ALKOXYBENZYLPIPERIDINE DERIVATIVE AS MELATONERGIC AGENT
Document Type and Number:
Japanese Patent JPH08208603
Kind Code:
A
Abstract:

To provide a new 3-alkoxybenzylpiperidine derivative useful as a therapeutic agent for sleep or circadian rhythm disorder of a patient, i.e. a melatonergic agent.

This 3-alkoxybenzylpiperidine derivative is expressed by formula I [R1 is a 1-4C alkyl, a 2-4C alkenyl, a 3-6C cycloalkyl or NR7R8 (R7 and R8 are each H or a 1-4C alkyl provided that R7 and R8 are not H at t e same time); R2 to R4 are each H or a 1-4C alkyl; R5 is H, a 1-4C alkyl, a halogen or CF3; R6 is a 1-4C alkyl; X is O or S; the phenylmethyl(benzyl) group is bonded to 3 or 4-position of the piperidine ring], e.g. 1-acetyl-4-[(2-fluoro-5- methoxyphenyl)methyl]piperidine. The compound of formula I can be produced e.g. by treating a pyridine of formula II (Y is CN or the like) with an organometallic reagent, hydrolyzing the product to obtain a ketone intermediate, successively subjecting the intermediate to reduction and the hydrogenation of the pyridine ring and using the obtained compound of formula III as an intermediate.


Inventors:
RONARUDO JIEI MATOSON
JIYON DEII KIYATSUTO
DANIERU JIEI KIIBUI
Application Number:
JP33356495A
Publication Date:
August 13, 1996
Filing Date:
December 21, 1995
Export Citation:
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Assignee:
BRISTOL MYERS SQUIBB CO
International Classes:
C07D211/18; A61K31/445; A61K31/451; A61P5/00; A61P25/20; A61P27/02; A61P27/06; A61P35/00; A61P37/04; A61P43/00; C07D211/16; C07D211/22; (IPC1-7): C07D211/22; A61K31/445; C07D211/18
Attorney, Agent or Firm:
Minoru Nakamura (6 outside)