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Method for preparing crystalline form 6 of Sofosbuvir

A non-buvir crystal form and crystallization technology, applied in the field of medicine, can solve the problems of unfeasible production, insufficient yield, large stirring resistance, etc., to avoid the use of flammable and explosive solvents, and the crystallization process. Simple and efficient, the effect of avoiding conversion steps

Inactive Publication Date: 2016-11-09
SHANGHAI SHYNDEC PHARMA HAIMEN CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, in the method disclosed in US8618076, method 1 has cumbersome steps, a long cycle, and does not have the feasibility of production; method 2 involves heterogeneous state transformation in water, and the process is difficult to control. Repeating the literature process found that the feed liquid during crystal transformation Extremely viscous, high stirring resistance, high requirements for equipment, and the yield is less than 80%
The method disclosed in the patent CN104829673 involves the use of ether solvents, which are flammable and explosive, and have great potential safety hazards in the production process

Method used

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  • Method for preparing crystalline form 6 of Sofosbuvir
  • Method for preparing crystalline form 6 of Sofosbuvir
  • Method for preparing crystalline form 6 of Sofosbuvir

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Mix 15g of sofosbuvir with 25g of methanol and 60g of water, heat to dissolve the solid completely; then cool to 20°C, and keep stirring for 2h; filter, and blow dry the filter cake at 55°C to obtain 13.5g of the product. Rate 90.0%. The XRPD pattern of the obtained sample is attached figure 1 shown.

Embodiment 2

[0029] Mix 15g of sofosbuvir with 20g of ethanol and 40g of water, heat to dissolve the solid completely, then cool to 15°C, keep stirring for 2h, filter, and dry the filter cake by blowing at 55°C to obtain 13.81g of the product. The rate is 92.07%.

Embodiment 3

[0031] Mix 15g of sofosbuvir with 25g of methanol and 80g of water, heat to dissolve the solid completely, then cool to 10°C, keep stirring for 4h, filter, and dry the filter cake by blowing at 55°C to obtain 14.2g of the product. The rate is 94.7%.

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PUM

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Abstract

The invention discloses a method for preparing crystalline form 6 of Sofosbuvir. The method comprises the following steps: 1) adding Sofosbuvir in a mixed solvent of an alcohols solvent and water, heating the material and dissolving the material; 2) cooling the solution obtained in the step 1) for crystallization; and 3) filtering the solid after crystallization and drying the solid to obtain crystalline form 6 of Sofosbuvir. Compared with the original preparation method of crystalline form 6, the crystallization technology of the present invention is used for preparing crystalline form 6 of Sofosbuvir, and the method has the advantages of high yield, loose product, easy drying, little application amount of the solvent, environmental protection and simple operation.

Description

technical field [0001] The invention relates to a preparation method of sofosbuvir crystal form 6, which belongs to the technical field of medicine. Background technique [0002] Sofosbuvir (also translated as Sofosbuvir, English name Sofosbuvir) is an inhibitor of HCVNS5B-dependent RNA polymerase invented by Gilead, USA, with a specification of 400 mg; the trade name is Sovaldi; the product was released on December 6, 2013. Launched in the US on 1st. Its molecular structural formula is as follows: [0003] [0004] Sofosbuvir is the first drug approved for the full oral treatment of hepatitis C. When used for the treatment of specific genotypes of chronic hepatitis C, it can eliminate the need for traditional injection drug interferon (IFN). Its 2014 The global sales volume exceeds 10 billion US dollars, and it has a broad market prospect. In November 2014, the US FDA approved Harvoni, a compound drug containing 400mg Sofosbuvir and 90mg Ledipasvir (another NS5B polym...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/10C07H1/06
CPCC07H19/10C07B2200/13C07H1/06
Inventor 严允兵于振鹏何康永张东亚谭兴志万国盛陈婷婷
Owner SHANGHAI SHYNDEC PHARMA HAIMEN CO LTD
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