反应详情

To 3.96 parts of 1-(4-fluorobenzoyl)aziridine, dissolved in 16 parts of benzene, are added 3.25 parts of 1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amine, 90 parts of benzene and 45 parts of N,N-dimethylformamide. The whole is stirred and refluxed for 5 hours. The reaction mixture is cooled and poured onto water. The layers are separated and the aqueous phase is extracted with methylbenzene. The combined organic phases are dried, filtered and evaporated. The residue is crystallized from a mixture of 2-propanone and 2,2'-oxybispropane, yielding 1part (19%) of 4-fluoro-N-[2-{4-[1-(4-fluorophenylmethyl)-1H-benzimidazol-2-ylamino]-1-piperidinyl}ethyl]benzamide; mp. 193.7° C.

1. temperaturerefluxed for 5 hours
2. temperatureThe reaction mixture is cooled
3. additionpoured onto water
4. customThe layers are separated
5. extractionthe aqueous phase is extracted with methylbenzene
6. customThe combined organic phases are dried
7. filtrationfiltered
8. customevaporated
9. customThe residue is crystallized from a mixture of 2-propanone and 2,2'-oxybispropane