反应详情

To a stirred solution of 248 parts of methyl 3-methyl-4-oxo-1-piperidinecarboxylate in 660 parts of acetic acid are added 150 parts of 4-fluorobenzenamine and the whole is stirred for 30 minutes. After cooling with ice-water, a solution of 69 parts of sodium cyanide in 195 parts of water is added dropwise at room temperature. Upon completion, stirring at room temperature is continued over week-end. The solid product is filtered off and washed with 2,2'-oxybispropane and petroleumether, yielding 230 parts of methyl 4-cyano-4-[(4-fluorophenyl)amino]-3-methyl-1-piperidinecarboxylate; mp. 90° C.

1. stirringUpon completion, stirring at room temperature
2. waitis continued over week-end
3. filtrationThe solid product is filtered off
4. washwashed with 2,2'-oxybispropane and petroleumether