PROCESS AND INTERMEDIATES FOR THE PREPARATION OF 4'-TRIFLUOROMETHYL-BIPHENYL-2-CARBOXYLIC ACID (1,2,3,4-TETRAHYDRO-ISOQUINOLIN-6-YL)-AMIDE
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,...
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Format: | Patent |
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Zusammenfassung: | 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 (C1C6)alkyl; R2 is selected from OR3, -CH2-NH2.(R5H)m, wherein m and R5H are defined below, and -CH2-NO2; or R1 and R2 together form an =O or =CH-NO2 group; with the proviso that when R1 and R2 are each an OR3 group then both R3s are (C1-C6)alkyl groups and the same. |
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