FREMGANGSMAADE TIL FREMSTILLING AF MEVALOLACTONANALOGE

摘要

Compounds of the general formula I where one of R and R0 is and the other is primary or secondary C1-6-alkyl, C3-6-cycloalkyl or phenyl-(CH2)2- , where R4 is hydrogen, C1-4-alkyl, trifluoromethyl, fluorine or chlorine, R5 is hydrogen, C1-3-alkyl, trifluoromethyl, fluorine or chlorine, and R5a is hydrogen, C1-2-alkyl, fluorine or chlorine, with the provisos that both R5 and R5a should be hydrogen if R4 is hydrogen, R5a should be hydrogen if R5 is hydrogen, and at most one of R4 and R5 is trifluoromethyl, R2 is hydrogen, C1-4-alkyl, C3-6-cycloalkyl, C1-4-alkoxy (except tert-butoxy), trifluoromethyl, fluorine, chlorine or benzyloxy, R3 is hydrogen or C1-3-alkyl, with the proviso that R3 should be hydrogen if R2 is hydrogen, X is -(CH2)n- or -CH=CH- (n = 1, 2 or 3), Z is where R6 is hydrogen or C1-3-alkyl, in the form of free acid or in the form of a physiologically hydrolysable and acceptable C1-3-alkyl, n- butyl, i-butyl, t-butyl or benzyl ester or a δ- lactone thereof or in the form of a salt, are prepared by a) if R6 is hydrogen, reducing a compound of the general formula V where R11 is a radical which forms a physiologically hydrolysable and acceptable ester, and X, R, Ro, R2 and R3 are as defined above, b) if R6 is C1-3-alkyl, hydrolysing a compound of the general formula XII where R6a is C1-3-alkyl, R12 is an ester-forming group, and X, R, Ro, R3 and R11 are as defined above, c) if X is -CH=CH-, deprotecting a compound of the general formula XXVIII where Pro is a protecting group, and R, Ro, R2 and R3 are as defined above, d) hydrolysing a compound of the general formula I in the form of a physiologically hydrolysable ester or lactone thereof, or e) esterifying or lactonizing a compound of the general formula I in free acid form, and, if a free carboxylic acid is present, the resulting compound is recovered in free form or in the form of a salt.