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A new crystal form of sofosbuvir and its preparation method

A technology of febuvir crystal form and crystal form, which is applied in the field of medicine, can solve the problems of unstable crystal form A, poor stability of crystal form A, poor fluidity, etc., and achieve excellent stability, good properties, good fluidity

Active Publication Date: 2020-09-22
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has been found through tests that the quality of the crystal form A is unstable, and some crystals are flaky solids with poor fluidity; and the crystal form stability of the crystal form A is not good, and it is easy to convert into form 6 during the preparation process

Method used

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  • A new crystal form of sofosbuvir and its preparation method
  • A new crystal form of sofosbuvir and its preparation method
  • A new crystal form of sofosbuvir and its preparation method

Examples

Experimental program
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Effect test

preparation example 1

[0055] Preparation Example 1: Preparation of Sofosbuvir Form 1 (refer to CN102858790A)

[0056] 2kg of sofosbuvir (prepared with reference to the disclosed method of CN102858790A, the same below) was dissolved in 10L of dichloromethane, then the solution was evaporated at 5°C, and after drying, 1.8kg of sofosbuvir in form 1 was obtained, with an HPLC purity of 99.4%.

preparation example 2

[0057] Preparation Example 2: Preparation of Sofosbuvir Form 6 (Refer to CN102858790A)

[0058] 500 g of sofosbuvir Form 1 was added to 20 L of deionized water, heated to 50 °C, and stirred vigorously for 1 h, during which time solids began to precipitate out of solution, forming a thin slurry. The slurry was cooled to 20 °C over 1.5 h and held at 20 °C for 16 h, then further cooled to 0-5 °C over 0.5 h and held at 0-5 °C for 2.5 h. The slurry was filtered on a medium porosity glass fritted funnel and washed with 5 L of ice-cold water. The wet cake was suction dried for 2 h, then vacuum dried at 50 °C for 23 h, and 440 g of Form 6 was isolated with an HPLC purity of 99.5%.

preparation example 3

[0059] Preparation Example 3: Preparation of Sofosbuvir Form A (refer to CN104130302A)

[0060] Weigh 570g of sofosbuvir, add 5L of acetone to dissolve, add 30L of n-pentane, and then leave it at room temperature for 16 hours in a closed room, and solids precipitate out. After filtration, the obtained solid was vacuum-dried at room temperature for 24 hours to obtain 500 g of solid, which was crystal form A, and the HPLC purity was 99.3%.

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Abstract

The invention discloses a new crystal form of sofosbuvir and a preparation method thereof. The powder X-ray diffraction of the new crystal form of sofosbuvir of the present invention has characteristic peaks at 2θ: 8.4±0.2°, 9.1±0.2°, 16.9±0.2°, 19.7±0.2°, 25.5±0.2°. The new sofosbuvir crystal form of the present invention has stable quality, stable crystal form, no hygroscopicity, and good fluidity. The preparation method is simple and suitable for industrialization, and is more suitable for storage and use as a raw material drug, and provides a method for the preparation of sofosbuvir medicine. new way.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a new crystal form of sofosbuvir and a preparation method thereof. Background technique [0002] Hepatitis C is a viral hepatitis caused by hepatitis C virus (HCV) infection, which can lead to chronic inflammation, necrosis and fibrosis of the liver, and some patients can develop liver cirrhosis or even hepatocellular carcinoma (HCC). extremely harmful to health and life. [0003] Hepatitis C is a global epidemic. According to the statistics of the World Health Organization, there are more than 200 million infected people in the world, and there are at least 3 to 4 million newly infected people every year. The current treatment for hepatitis C is mainly immunotherapy with recombinant α-interferon alone or combined with ribavirin, a nucleoside analogue, and the clinical effect is limited. [0004] Sofosbuvir (Sofosbuvir) is a new drug developed by Gilead Pharmaceuti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H19/10C07H1/06A61K31/7072A61P31/14
CPCC07B2200/13C07H1/06C07H19/10
Inventor 李志怀陈玉洁金凯底辉峰刘洋赫玉霞张丹丹刘春玲刘晓争马玉秀
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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