| 摘要 |
<p>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-CHR1R2 wherein A is a group of formula (XII) and R1 selected from H and OR3 wherein R3 is hydrogen or (C¿1?-C6)alkyl; R?2¿ is selected from OR3, -CH2-NH2.(R5H)m, wherein m and R5H are defined below, and -CH¿2?-NO2; or R?1 and R2¿ together form an =O or =CH-NO¿2? group; with the proviso that when R?1 and R2¿ are each an OR3 group then both R3s are (C¿1?-C6)alkyl groups and the same.</p> |
