abstract |
Benzocycloalkenyl dihydroxy alka- acid derivatives noïiques, HMG CoA reductase inhibitors, antagonists thromboxane A2 receptors and antifungals, shown by formula 1 in which, X = CH2, O or S; R1 and R2 identical or different = H, C1-3 alkyl or together form a chain - (CH2) n- (n = 4.5) optionally substituted sym-trically with one or two C1-3 alkyl radicals. R3 and R4 identical or different = H, CF3, halogen (Cl, F, Br), N, N-C1-5 dialkylamino, C1-4 alkyl, C1-5 alkoxy, C1-3 alkylthio, or phenyl optionally substituted by at most two substituents which may be the same or different and represent radicals, C1-3 alkyl, C1-3 alkoxy, or halogens (F, Cl) provided that when one of R3, R4 represents the radicals: CF3, N, N-dialkylamino, C6H5, or substituted phenyl, it is found on vertices 3 ', 4', or 5 'according to formula 1 and the other denotes a hydrogen atom. R5 and R6 (which can be identical or different) = H, halogen (F, Cl, Br), CF3, C1-3 alkyl, C1-3 alkoxy, C6H5, optionally substituted by up to two substituents which may be identical or different and represent radicals C1-3 alkyl, C1-3 alkoxy or halogen atoms (F, C1), provided that when one of R5, R6 = CF3, C6H5 or substituted phenyl, it sits on top 6 or 7 and the other denotes a hydrogen atom. The R3 substituents and R4 respectively R5 and R6 can also form together, provided they are on two adjoining peaks, the diradicals of formulas: -CH = CH-CH = CH-, - (CH2) m-, -O (CH2) pO-, in which m = 3 or 4, p = 1 or 2, being understood that when R3 and R4 respectively R5 and R6 form the sequence -O (CH2) pO-, this is linked to vertices 3 ', 4' or 4 ', 5' respectively 6, 7 depending on the formula 1. R7 and R8 = H or form together with the liai-its existing CC a double bond of trans geometry; R9 and R10 = H or together form a dialkylmethylene residue in C1-3. In the form of free acids, salts, esters, amides, or .delta.-lactones. Hypocholeste-rolemic, antithrombotic and antifungal nant. Intermediaries used in the preparation of compounds of formula 1 as well as process for the preparation of these latter. |