Method for producing 3-(4-piperidinyl)-2,3,4,5-tetrahydro-1,3-benzodiazepin-2(1H)-one

摘要

Disclosed is a process for preparing the compound of formula (I) characterised in that (a) 2-nitrophenylacetic acid is reacted with 4-amino-N-phenylmethylpiperidine in the presence of condensing agents; (b) the carbonyl group of the resulting 2-nitro-N-[1-(phenylmethyl)-4-piperidinyl]-phenylacetamide is converted into a methylene group by the addition of a reducing agent; (c) after reduction of the nitro group in the presence of a Raney nickel catalyst, the intermediate product N-[2-(2-nitrophenyl)ethyl]-1-(phenylmethyl)-4-amino-piperidine obtained is cyclised by the addition of condensing agents to obtain 3-[1-(phenylmethyl)-4-piperidinyl]-2,3,4,5-tetrahydro-1,3-benzodiazepin-20 2(1H)-one and (d) by cleaving the benzyl protecting group the 3-[1-(phenylmethyl)-4-piperidinyl]-2,3,4,5-tetrahydro-1,3-benzodiazepin-2(1H)-one is converted into the compound of formula (I).