Method for preparing acid ethyl ester (22.45) - 4 - (3,5-bis (trifluoromethyl - - Methoxycarbonyl benzyl) amino ethyl - 2 - 6 - trifluoromethyl - 3,4-dihydro - 2H - quinoline - 1 - carboxylic acid anhydrous

摘要

1. Preparation of ester (2R, 4S) - 4 - [(3, 5-bis-trifluorometil-bencil) - methylamine] - 2-ethyl-6-trifluoromethyl-3, 4-dihydro-2h-quinolin-1-carboxylico anhydro de form (1),It includes: combining ethyl ester (2R, 4S) - 4 - [(3, 5-bis-trifluoro-benzene) - methoxy-amine] - 2-ethyl-6-trifluoro-trifluoro-3, 4-dihydro-2h-quinine-1-carboxy with a solvent at a temperature sufficient to dissolve the ethyl ester (2R, 4S) - 4 - [(3), 5-bis-trifluoro-metal-bencil) - metaloxicarbonil-amine] - 2-ethyl-6-trifluoro methyl-3, 4-dihydro-2h-quinlin-1-carboxyl for a solution, which fall includes heptanos or a composite of water and a pol;2. [(3,5-bis-trifluorometarbone-amine] - 2-ethyl-6-trifluorometarbone-3,4-dihydro-2h-quinlin-1-carboxyl-solid, including the formation to cool or evaporate the solution so that the solvent in the solution is sufficient to form the ethyl acetate (2R, 4S) - 4 - [(3), 5-bis-trifluoro-metallic-bencil) - methoxicarbone amine] - 2-ethyl-6-trifluoro-metallic-3, 4-dihydro-2h-quinlin-1-carboxyl solid;2. The ethyl ester was separated from acid (2R, 4S) - 4 - [(3, 5-bis-trifluoromethyl-bencil) - metrobonil-amine] - 2-ethyl 6-trifluoromethyl-3, 4-dihydro-2h-quinlin-1-carboxyl in solid solvent to obtain Ethyl Acid (2R, 4S) - 4 - [(3, 5-bis-trifluoromethyl-bencil) - amine-3] - trifluoroethane] - 3; 4-dihydro-2H-quinolin-1-anhydro carboxyl. These compounds are inhibitors of cholesterol ester transfer proteins.