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Rosuvastatin intermediate, preparation method of intermediate and preparation method of rosuvastatin ester

A technology for rosuvastatin and intermediates, applied in the field of compound and compound synthesis, can solve the problems of cumbersomeness, low reaction efficiency, cumbersome steps, etc., and achieve the effect of simplifying the synthesis process steps, reducing the generation of impurities, and realizing industrial production

Pending Publication Date: 2022-01-14
宣城美诺华药业有限公司
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Problems solved by technology

However, in the existing process of synthesizing rosuvastatin calcium, it generally needs to be oxidized first and then replaced. Impurities are easily produced during the reaction process, and cumbersome separation and purification steps are required. The steps are cumbersome and the reaction efficiency is low.

Method used

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  • Rosuvastatin intermediate, preparation method of intermediate and preparation method of rosuvastatin ester

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Embodiment Construction

[0051] The present invention will be further described in detail below in conjunction with the accompanying drawings and embodiments.

[0052] The code name of the rosuvastatin intermediate in this example is RST-Z11, and the name is N-(5-(((1-benzyl-1H-benzo[d]imidazol-2-yl)-sulfone)-methyl )-4-(4-fluorophenyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide is a new compound, affected by the group and structure of the compound itself, The substituent can promote the reaction and reduce the generation of impurities, which provides conditions for the "one-step" preparation of rosuvastatin ester.

[0053] The molecular formula of compound RST-Z11 is C 30 h 30 FN 5 o 4 S 2 , the structural formula is:

[0054]

[0055] The preparation method of above-mentioned rosuvastatin intermediate is:

[0056] (1) Synthesis of compound RST-Z7

[0057] In 800mL of tetrahydrofuran, add 40g of anhydrous magnesium chloride and 22.7g of potassium borohydride, heat to reflux (abo...

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Abstract

The invention relates to a rosuvastatin intermediate, a preparation method of the intermediate and a preparation method of rosuvastatin ester, and provides a novel rosuvastatin intermediate compound, namely, N-(5-(((1-benzyl-1H-benzo [d] imidazole-2-yl)-sulfone)-methyl)-4-(4-fluorophenyl)-6-isopropylpyrimidine-2-yl)-N-methylmethanesulfonamide. The rosuvastatin intermediate can be used for synthesizing rosuvastatin ester, under the influence of the self structure of the rosuvastatin intermediate, when the rosuvastatin ester is synthesized, a substitution reaction can be carried out firstly, and then an oxidation reaction is carried out, and the generation of impurities in the reaction process is reduced, so that the reaction can be carried out through a 'one-step method', the synthesis process steps are greatly simplified, and the industrial production of the rosuvastatin ester is favorably realized.

Description

technical field [0001] The invention relates to the technical field of compound and compound synthesis, and specifically refers to a rosuvastatin intermediate, a preparation method of the intermediate and a preparation method of rosuvastatin ester. Background technique [0002] Rosuvastatin calcium, chemical name: bis-[E-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]-pyrimidine-5 -yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid]calcium salt (2:1), is an IMG-CoA inhibitor developed by AstraZeneca for the treatment of heart disease Vascular disease, with the characteristics of strong potency, high safety and few side effects, plays an important role in the treatment of cardiovascular diseases. [0003] The synthesis of rosuvastatin calcium from rosuvastatin ester is a commonly used synthesis method of rosuvastatin calcium in the prior art. For example, the compound 6-[(1E)-2-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]-5-pyrimidine]vinyl]- 2,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/12C07D405/06
CPCC07D403/12
Inventor 余奎唐雪松周国斌黄想亮曹倩姚成志
Owner 宣城美诺华药业有限公司
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