TERTIARY BUTYL-(E)-(6-{2-[4-(4-FLUOROPHENYL)-6-ISOPROPYL-2-[METHYL(METHYLSULFONYL)AMINO]-PYRIMIDINE-5-YL}-(4R,6S)-2,2-DIMETHYL[1,3]DIOXANE-4-YL]ACETATE AND METHOD FOR ITS PREPARING, DIPHENYL-[4-(4-FLUOROPHENYL)-6-ISOPROPYL-2-[METHYL(METHYLSULFONYL)AMINO]-PYRIMIDINE-5-YLMETHYL]PHOSPHINE OXIDE, METHODS FOR PREPARING (E)-7-[4-(4-FLUOROPHENYL)-6-ISOPROPYL-2-[METHYL(METHYLSULFONYL)AMINO]-PYRIMIDINE-5-YL]-(3R,5S)-3,5-DIHYDROXYHEPT-6-ENOIC ACID AND ITS DERIVATIVES Russian patent published in 2005 - IPC

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to an intermediate compound, i. e. tert.-butyl-(E)-(6-{2-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]-pyrimidine-5-yl}-(4R,6S)-2,2-dimethyl[1,3]dioxane-4-yl]acetate that can be used in synthesis of compound of the formula (IV)

eliciting inhibitory effect on activity of HMG-CoA-reductase and, therefore, can be used for preparing pharmaceutical agents for treatment, for example, hypercholesterolemia, hyperproteinemia and atherosclerosis. Also, invention relates to a method for preparing indicated intermediate compound by reaction of the new parent compound - diphenyl-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidine-5-ylmethyl]phosphine oxide with tert.-butyl-2-[(4R,6S)-6-formyl-2,2-dimethyl-1,3-dioxane-4-yl]acetate in the presence of a strong base in simple ether or aromatic solvents or their mixtures at temperature in the range from -20⁰C to -90⁰C. Also, invention relates to a method for preparing of compound of the formula (IV) wherein R¹ means hydrogen atom or pharmaceutically acceptable cation and to a method for preparing intermediate compounds of the formula (VI):

wherein each P¹ and P² represents independently (C₁-C₄)-alkyl or group:

and wherein P³ represents (C₁-C₈)-alkyl. Applying new intermediate compounds and proposed methods provide enhancing quality and yield of compounds.

EFFECT: improved preparing methods.

9 cl, 1 tbl, 8 ex