| 摘要 |
An improved process, and intermediates, for the preparation of 4'-trifluoromethyl-biphenyl-2-carboxylic acid (1,2,3,4-tetrahydro-isoquinolin-6-yl)-amide (I). Compound (I) is useful in the preparation of 4'-trifluoromethyl-biphenyl-2-carboxylic acid [2-(1H-[1,2,4-triazol-3-ylmethyl)]-(1,2,3,4-tetrahydro-isoquinolin-6-yl)-amide (II) which is useful as an inhibitor of microsomal triglyceride transfer protein and/or apolipoprotein B (Apo B) secretion, and which are accordingly useful for the preparation and treatment of atherosclerosis and its clinical sequelae, for lowering serum lipids, and related diseases. A compound of the formula A-CHR<1>R<2> wherein A is a group of formula (XII) and R<1> selected from H and OR<3> wherein R<3> is hydrogen or (C1-C6)alkyl; R<2> is selected from OR<3>, -CH2-NH2.(R<5>H)m, wherein m and R<5>H are defined below, and -CH2-NO2; or R<1> and R<2> together form an =O or =CH-NO2 group; with the proviso that when R<1> and R<2> are each an OR<3> group then both R<3>s are (C1-C6)alkyl groups and the same.
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