2-(1-Benzyl-4-hydroxypiperidin-4-yl)acetaMide synthesis

Yield:28530-95-2 30%

Reaction Conditions:

with methanol;ammonia at 100; for 72 h;

Steps:

17.a

A solution of ethyl [4-hydroxy-1 -(phenylmethyl)-4-piperidinyl]acetate (15 g, 54.15 mmol) [prepared according to Caroon, J. M.; et al. J. Med. Chem. 1981, 24, 1320.] in 7N NH₃-MeOH (16 mL) was heated to 100⁰C in a sealed tube for 3d. The solution was cooled and concentrated and the residue washed with DCM providing the title compound (4g, 30%) as a white solid which was used directly without further purification : LCMS (ES) m/e 249 (M+H)⁺.

References:

WO2006/81289,2006,A2 Location in patent:Page/Page column 38