Amino acid salt of antihypercholesterolemia tetrazole compound and its production

PURPOSE: To obtain a novel tetrazol compound useful as an HMG-CoA reductase inhibitor and for treatment of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis. CONSTITUTION: A compound represented by formula I [wherein R 1 and R 4 are each H, a halogen, a 1-4C alkyl, trifluoromethyl, or the like; R 2 , R 3 , R 5 and R 6 are each H, a halogen, a 1-4C alkyl, or a 1-4C alkoxy; R 7 is an amino acid; tet is formula II or III (wherein R 8 is H, a 1-4C alkyl, a 1-4C alkoxy, or the like)] is produced. Examples thereof include [4R-[4a, 6b(E)]]-6-[4,4-bis(4- fluorophenyl)-3-(1-methyl-1H-tetrazol-5-yl)-1,3-butadienyl]-tetrahydro-4-hydroxy-2H- pyran-2-one. A compound represented by formula IV is reacted with a compound represented by formula V in the presence of a condensing agent. The product is reacted with an acid, then reacted with a base, and further, reacted with an acid so as to provide a compound represented by formula VI. This compound is reacted with cinchonidine. The product is reacted with a coupling reagent or an activating agent to obtain the objective compound represented by formula I. COPYRIGHT: (C)1995,JPO