Triethylamine → (2R,4S)-N-[1-(3,5-Bis-trifluoromethyl-benzoyl)-2-benzyl-piperidin-4-yl]-quinazoline-4-carboxamide

Participants

Reaction Steps

Analogously to Example 1, 252 mg (1.45 mmol) of (2R,4S)-2-benzyl-1-(3,5-bis-trifluoromethyl-benzoyl)-4-piperidineamine in 5 ml of methylene chloride are reacted with 368 mg (1.45 mmol) of bis(2-oxo-3-oxazolidinyl)phosphinic acid chloride, 440 mg (4.35 mmol) of triethylamine and 566 mg (1.32 mmol) of quinazoline-4-carboxylic acid. The title compound is obtained in the form of white crystals. M.p.: 92-172° C.; TLC: hexane/ethyl acetate (1:1) Rf =0.37, FD-MS: M+ =586; [alpha]D=+1.3 (c=0.98, methylene chloride). ##STR16##

Provenance & Evidence