PROCESS FOR PREPARING 1-(4-PIPERIDINYL)BENZIMIDAZOLONE DERIVATIVES

摘要

Provided is a process for preparing 1-(4-piperidinyl)- benzimidazolone derivatives industrially in a high yield and at a low cost. Specifically provided is a process for preparing 1-(4-piperidinyl)benzimidazolone derivatives (1) or salts thereof, which comprises the following steps: step (1) of preparing a compound (4) by reductive amination of a piperidone (2) with an aniline (3); and step (2) of reacting the compound (4) with di-t-alkyl dicarbonate or N,N'-disuccinimidyl carbonate to prepare a 1-(4-piperidinyl)benzimidazolone derivative (1). In reaction formula [ I ], R1 is an optionally substituted alkyl group or an optionally substituted cyclic group; and R2 is an optionally substituted alkyl group, an optionally substituted alkenyl group, or an optionally substituted aryl group.