反应详情

To a stirred mixture of 55 parts of 2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-1H-benzimidazole and 450 parts of N,N-dimethylformamide were added 10.6 parts of a sodium hydride dispersion 50% and stirring was continued for 1 hour. Then there were added dropwise 26 parts of 1-(chloromethyl)-4-fluorobenzene (slightly exothermic reaction). Upon completion, stirring was continued overnight at room temperature. Water was added and the product was extracted with 4-methyl-2-pentanone. The extract was dried, filtered and evaporated. The solid residue was stirred in 1,1'-oxybisethane. The product was filtered off and dried, yielding 67.6 parts (90%) of 1-[(4-fluorophenyl)methyl]-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-1H-benzimidazole; mp. 127.5° C. (34).

1. customslightly exothermic reaction)
2. stirringUpon completion, stirring
3. waitwas continued overnight at room temperature
4. extractionthe product was extracted with 4-methyl-2-pentanone
5. customThe extract was dried
6. filtrationfiltered
7. customevaporated
8. stirringThe solid residue was stirred in 1,1'-oxybisethane
9. filtrationThe product was filtered off
10. customdried