3-(PIPERIDIN-4-YL)BENZONITRILE HYDROCHLORIDE synthesis

Yield:-

Reaction Conditions:

in 4-(dicyanomethylene)-2-methyl-6-(p-dimethylaminostyryl)-4H-pyran;trifluoroacetic acid at 20; for 1.25 h;

Steps:

13.C INTERMEDIATE 13

Step C: A solution OF TERT-BUTYL 4- (3-CYANOPHENYL) PIPERIDINE-1-CARBOXYLATE (376mg, 1. 31mmol) in lOmL of 1: 1 TFA/DCM was stirred at rt for 1.25h. The reaction mixture was concentrated. Purification by preparative TLC (silica, 1% of 28% NH40H solution/9% METHANOL/DCM) gave 3- PIPERIDIN-4-YLBENZONITRILE as a white solid. ESI-MS calc. for C12H14N2 : 186; Found: 187 (M+H).

References:

WO2004/92124,2004,A2 Location in patent:Page 82