An improved sofosbuvir preparation method

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A compound, Lewis acid technology, applied in the field of medicine and chemical industry, can solve problems such as unsafe

Active Publication Date: 2017-02-15

SUNSHINE LAKE PHARM CO LTD

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Problems solved by technology

The scheme provided by the present invention does not use flammable and explosive tert-butylmagnesium chloride, has the advantages of mild reaction conditions, convenient reagent storage, safe use, easy operation, convenient post-treatment, etc., and is easy to realize large-scale production of raw materials in factories, overcoming existing problems. There are disadvantages that the method of synthesizing Sofosbuvir is not safe

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[0034] Specifically, the improved sofosbuvir preparation method of the present invention may include:

[0035] a) adding compound I, compound II, Lewis acid and organic solvent into the reaction vessel, and adding alkali;

[0036] b) Control the reaction temperature of the system at 20°C to 40°C, and stir the reaction until the compound I content is ≤3.0%;

[0037] c) stop the reaction, extract the reaction solution, and then perform crystallization to obtain compound III.

[0038] Specifically, the method for preparing the improved sofosbuvir described in the present invention may include the following steps:

[0039] a) adding compound I, compound II, Lewis acid and organic solvent into the reaction vessel, and adding alkali;

[0040] b) Control the reaction temperature of the system at 20°C to 40°C, and stir the reaction until the compound I content is ≤3.0%;

[0041] c) Stop the reaction, extract the reaction solution with dichloromethane, wash with aqueous sodium carbo...

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[0081] In order to enable those skilled in the art to better understand the technical solutions of the present invention, some non-limiting examples are further disclosed below to further describe the present invention in detail.

[0082] The reagents used in the present invention can be purchased from the market or can be prepared by the methods described in the present invention.

[0083] In the present invention, ml or mL refers to milliliter, L refers to liter, g refers to gram, kg refers to kilogram, mol / L refers to mole / liter, h refers to hour, min refers to minute, v / v refers to volume ratio,

[0084] HPLC detection chromatographic conditions are as follows:

[0085] Chromatographic column: Waters XSELECT HSS T3 (4.6*100mm, 2.5um);

[0086] Flow rate: 1.5mL / min; Detection wavelength: 210nm; Column temperature: 25°C;

[0087] Running time: 29min; Injection volume: 2μl;

[0088] Mobile phase: Phase A: Dissolve 0.5mL of ...