PROCESS FOR PREPARING 1-(4-PIPERIDINYL)BENZIMIDAZOLONE DERIVATIVES
申请人:Mitsubishi Tanabe Pharma Corporation
公开号:EP2394997A1
公开(公告)日:2011-12-14
Provision of an industrial method of producing a 1-(4-piperidinyl)benzimidazolone derivative in a high yield at a low cost.
A production method of 1-(4-piperidinyl)benzimidazolone derivative (1) or a salt thereof according to the following steps.
[step 1] a step of subjecting a piperidone compound (2) and an aniline compound (3) to a reductive amination reaction to give a compound (4)
[step 2] a step of reacting the compound (4) with di-t-alkyl dicarbonate or N,N'-disuccinimidyl carbonate to give the 1-(4-piperidinyl)benzimidazolone derivative (1)
wherein R1 is optionally substituted alkyl or an optionally substituted cyclic group, and
R2 is optionally substituted alkyl, optionally substituted alkenyl or optionally substituted aryl.