4-(3,4-difluorophenyl)piperidine hydrochloride synthesis

Yield:262272-56-0 30%

Reaction Conditions:

with hydrogen;palladium over charcoal in ethanol; under 2585.81 Torr; for 15 h;

Steps:

4

Example 4:4-(3,4-DIFLUOROPHENYL)PIPERIDINEA mixture of 4-(3,4-difluorophenyl)-l,2,3,6-tetrahydropyridine (7.5 g, 38.4 mmol) and palladium on carbon (1.36 g) in ethanol (30 ml) was hydrogenated at 50 psi for 15 h under hydrogen. The reaction mixture was filtered through a pad of celite and the filtrate was concentrated and evaporated to dryness to give 4.86 g of crude product. Purification by flash column chromatography (ethyl acetate/methanol 1 : 1) gave the title compound (2.3 g, 30%). The amine was converted to the hydrochloric acid salt and recrystallized from ethanol/diethyl ether: M. p. 255-256 ⁰C. MS m/z (relative intensity, 70 eV) 197 (M+, 72), 196 (39), 140 (22), 127 (23), 56 (bp).

References:

WO2007/65655,2007,A1 Location in patent:Page/Page column 25