A method for preparing rosustatin and pitavastatin 2,6-diene enanthate compound

Abstract

The invention discloses a method for preparing rosustatin and pitavastatin 2,6-diene enanthate compound, which comprises (4R,6S)-6-[(1E)-2-[4-(4- Fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]-5-pyrimidine]vinyl]-2,2-dimethyl-1,3-dioxane-4 ‑tert-butyl acetate and (4R,6S)‑6‑[[(1E)‑2‑cyclopropyl‑4‑(4‑fluorophenyl)‑3‑quinolyl]vinyl]‑2,2‑ Dimethyl-1,3-dioxane-4-tert-butyl acetate was used as the starting material of rosuvastatin and pitavastatin respectively, and statinic acid was prepared by deprotection and hydrolysis in one step; As the reaction substrate, the 2,6-diene heptanoate compound was prepared through two steps of dehydration and substitution. The preparation and synthesis routes of rosuvastatin and pitavastatin 2,6-diene heptanoate involved in the present invention are short and easy to operate, easy to operate, high in product yield, and more suitable for large-scale industrial production.

Description

technical field

[0001] The invention relates to the field of drug synthesis, in particular to a method for preparing rosustatin and pitavastatin 2,6-diene enanthate compounds. Background technique

[0002] Rosuvastatin Calcium is the latest statin drug approved by AstraZeneca in Europe in 2002 for the treatment of primary and familial hypercholesterolemia and mixed dyslipidemia. It was approved for marketing in the United States in August 2003, thus becoming the seventh statin drug to enter the market. Its chemical name is: (3R,5S,6E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonamido)-5- Calcium pyrimidine]-3,5-dihydroxy-6-heptenoate. The structure looks like this:

[0003]

[0004] Pitavastatin Calcium is a third-generation statin lipid-lowering drug jointly developed and produced by Nissan Chemical Industry Co., Ltd. and Kowa Co., Ltd. This product has been launched in Japan in October 2003, and it is used for the treatment of primary hypercholestero...

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