PROCESS FOR PRODUCING MEVINIC ACID DERIVATIVES AND PHARMACEUTICAL PREPARATIVES CONTAINING THESE COMPOUNDS

摘要

Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula wherein: R<1>, R<2> and R<3> are independently selected from: (1) alkyl, (2) substituted alkyl in which one or more substituents are selected from (a) halogen, (b) hydroxyl, (c) alkoxy, (d) alkoxycarbonyl, (e) acyloxy, (f) cycloalkyl, (g) phenyl, (h) substituted phenyl in which one or more substituents are X or Y, (i) alkyl-S(O)n, (j) cycloalkyl-S(O)n, (k) phenyl-S(O)n, (l) substituted phenyl-S(O)n in which one or more substituents are X or Y, and (m) oxo, (3) alkoxy, (4) alkenyl, (5) cycloalkyl, (6) substituted cycloalkyl in which one or more substitutents are selected from (a) alkyl, (b) substituted alkyl in which one or more substituents are selected from (i) halogen, (ii) hydroxy, (iii) alkoxy, (iv) alkoxycarbonyl (v) acyloxy (vi) phenyl (vii) substituted phenyl in which one or more substituents are X and Y, (viii) alkyl-S(O)n, (ix) cycloalkyl-S(O)n, (x) phenyl-S(O)n (xi) substituted phenyl-S(O)n in which one or more substituents are X and Y, and (xii) oxo, (c) alkyl-S(O)n, (d) cycloalkyl-S(O)n, (e) phenyl-S(O)n, (f) substituted phenyl-S(O)n in which one or more substituents are X or Y, (g) halogen, (h) hydroxy, (i) alkoxy, (j) alkoxycarbonyl, (k) acyloxy, (l) phenyl, and (m) substituted phenyl in which one or more substituents are X and Y, (7) phenyl, (8) substituted phenyl in which one or more substituents are X or Y, (9) amino, (10) alkylamino, (11) dialkylamino, (12) phenylamino, (13) substituted phenylamino in which one or more substituents are X or Y, (14) alkyl(substituted phenyl)amino in which one or more substituents are X and Y, (15) phenylalkylamino, (16) di(phenylalkyl)amino, (17) substituted phenylalkylamino in which one or more substituents are X or Y, (18) a member selected from (a) piperidinyl, (b) pyrrolidinyl, (c) piperazinyl, (d) morpholinyl, (e) thiomorpholino, (f) histaminyl, (g) 3-aminomethyl pyridinyl, and (19) hydroxy substituted alkylamino; X and Y are independently hydrogen, halogen, trifluoromethyl, alkyl, nitro, alkoxy, or cyano; n is 0, 1, or 2; M+ is hydrogen, ammonium, or an alkali metal. o