3-PIPERIDIN-4-YL-BENZOIC ACID METHYL ESTER HCL synthesis

Yield: 74%

Reaction Conditions:

with hydrogenchloride at 20;

Steps:

A.A15 EXAMPLE A15 [0488] Methyl 3-(4-piperidinyl)-benzoate-hydrochloride
The mixture of 500 mg (2.069 mmol) of 3-(4-piperidinyl)-benzoic acid-hydrochloride and 10 ml saturated methanolic hydrogen chloride solution was stirred overnight at room temperature. The reaction mixture was concentrated by evaporation in vacuo, the residue was stirred with 3 ml isopropanol, suction filtered, washed with diethyl ether and dried at 60° C. in the circulating air dryer. 390 mg (74% of theory) of colourless crystals were obtained, Rf 0.34 (EI D). [0490] IR (KBr): 1728 (CO) cm-1 [0491] ESI-MS: (M+H)+=220; [0492] (M+Cl+HCl)=290/292/294 (Cl2)

References:

Boehringer Ingelheim International GmbH US2004/192729, 2004, A1 Location in patent:Page 32