Method for preparing rosuvastatin and pitavastatin 2, 5-diene heptanoate compound

A technology of diene enanthate and pitavastatin, which is applied in the field of preparation of rosustatin and pitavastatin 2,5-diene enanthate compound, which can solve the problems of expanding the application of drugs, complicated process routes, Poor operability and other problems, to achieve the effect of short and easy synthetic route, high product yield and easy operation
CN111100075AActive Publication Date: 2020-05-05NANTONG CHANGYOO PHARMATECH CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
NANTONG CHANGYOO PHARMATECH CO LTD
Publication Date
2020-05-05

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Abstract

The invention discloses a method for preparing rosuvastatin and pitavastatin 2, 5-diene heptanoate compound. (4R, 6S)-6-[(1E)-2-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl (methanesulfonyl)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 are respectivelytaken as starting materials of rosuvastatin and pitavastatin, deprotection and a hydrolyzation one-step method is adopted to prepare statin acid, then the statin acid is taken as a reaction substratefor dehydration and substitution two-step reaction to prepare the 2, 5-diene heptanoate compound. The preparation and synthesis routes of rosuvastatin and pitavastatin 2, 5-diene heptanoate involved in the invention are short and feasible, the operation is simple and convenient, the product yield is high, and the rosuvastatin and pitavastatin 2, 5-diene heptanoate is more suitable for large-scaleindustrial production.
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Description

technical field

[0001] The invention relates to the field of drug synthesis, in particular to a method for preparing rosustatin and pitavastatin 2,5-diene heptanoate 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 hypercholester...

Claims

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