Thiophene → 1-[3-[4-[2-(4-fluorophenyl)-2-oxoethyl]-1-piperidinyl]butyl]-1,3-dihydro-2H-benzimidazol-2-one

Participants

Reaction Steps

To 1 part of a volume of 2 parts of thiophene in 40 parts of ethanol are added 4.1 parts of 1,3 -dihydro-1-(3-oxobutyl)-2H-benzimidazol-2-one, 5.2 parts of 1-(4-fluorophenyl)-2-(4-piperidinyl)ethanone hydrochloride, 2 parts of sodium hydrogen carbonate and 160 parts of methanol. The whole is hydrogenated in the Parr-apparatus at 60° C. with 2 parts of palladium-on-charcoal catalyst 10%. After the calculated amount of hydrogen is taken up, the catalyst is filtered off and the filtrate is allowed to crystallize. The product is filtered off and dried, yielding 2.7 parts (33%) of 1-[3-[4-[2-(4-fluorophenyl)-2-oxoethyl]-1-piperidinyl]butyl]-1,3-dihydro-2H-benzimidazol-2-one; mp. 185.4° C.

Provenance & Evidence