Tenofovir alafenamide fumarate raw material medicine and production process thereof

A technology of tenofovir fumarate and alafenamide, which is applied in the field of medicine to achieve enhanced anti-hepatitis B effect and excellent anti-hepatitis B effect

Inactive Publication Date: 2018-07-20
安徽安科恒益药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, the treatment cost of hepatitis B patients is also a great social burden and family burden. Hepatitis B is st

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] A kind of tenofovir alafenamide fumarate raw material medicine, the manufacture raw material of described tenofovir alafenamide fumarate raw material comprises anhydrous tenofovir, triphenyl phosphite, 4- Dimethylaminopyridine, triethylamine, acetonitrile, ethyl acetate, methanol, concentrated hydrochloric acid, thionyl chloride, toluene, dichloromethane, L-alanine isopropyl hydrochloride, potassium bicarbonate, fumaric acid and isopropanol, the raw materials and auxiliary materials for the production of tenofovir alafenamide fumarate bulk drug are lactose monohydrate, microcrystalline cellulose, croscarmellose sodium and magnesium stearate, and the rich The mass parts of raw materials and auxiliary materials for the manufacture of tenofovir alafenamide maleate raw materials are 0.36 parts of anhydrous tenofovir, 0.68 parts of triphenyl phosphite, 0.10 parts of 4-dimethylaminopyridine, and 0.10 parts of triethylaminopyridine. 0.13 parts of amine, 3.00 parts of acetonitr...

Embodiment 2

[0035] A tenofovir alafenamide fumarate bulk drug, characterized in that: the manufacturing raw materials of the tenofovir alafenamide fumarate bulk drug include anhydrous tenofovir, triphenyl phosphite Esters, 4-dimethylaminopyridine, triethylamine, acetonitrile, ethyl acetate, methanol, concentrated hydrochloric acid, thionyl chloride, toluene, dichloromethane, L-alanine isopropyl hydrochloride, potassium bicarbonate , fumaric acid and isopropanol, the raw materials and auxiliary materials for the production of tenofovir alafenamide fumarate bulk drug are lactose monohydrate, microcrystalline cellulose, croscarmellose sodium and magnesium stearate , the mass parts of the manufacturing raw materials and auxiliary materials of tenofovir alafenamide fumarate bulk drug are 0.40 parts of anhydrous tenofovir, 0.72 parts of triphenyl phosphite, 0.20 parts of 4-dimethylaminopyridine Parts, 0.24 parts of triethylamine, 3.30 parts of acetonitrile, 5.38 parts of ethyl acetate, 2.9 part...

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Abstract

The invention discloses a tenofovir alafenamide fumarate raw material medicine and a production process thereof. The tenofovir alafenamide fumarate raw material medicine includes anhydrous tenofovir,triphenyl phosphite, 4-dimethylaminopyridine, triethylamine, acetonitrile, ethyl acetate, methanol, concentrated hydrochloric acid, thionyl chloride, toluene, dichloromethane, L-alanine isopropyl ester hydrochloride, potassium hydrogencarbonate, fumaric acid and isopropanol. Production raw material excipients for the tenofovir alafenamide fumarate raw material medicine include lactose monohydrate,microcrystalline cellulose, croscarmellose sodium and magnesium stearate. The new manufacturing raw materials and the production raw material excipients are selected, so that the anti-hepatitis B effect of the medicine is more excellent, mass production can be performed through the novel production method, and the anti-hepatitis B effect is strengthened to some extent.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a raw material drug of tenofovir alafenamide fumarate and a production process thereof. Background technique [0002] Now our country is still a big country with hepatitis B, and there are many patients, and there is no way to cure hepatitis B at present. For patients, there is an urgent need for antiviral drugs with better efficacy and fewer side effects. At present, the hepatitis B drugs on the market are more or less drug-resistant, and the needs of patients for better treatment are far from being met. [0003] Hepatitis B brings not only physical pain, but also psychological pain to patients, because discrimination against hepatitis B patients is common in society, which will have a great impact on patients' making friends, life, study, and employment. Moreover, the treatment cost of hepatitis B patients is also a great social burden and family burden. Hepatitis B is still ...

Claims

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Application Information

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IPC IPC(8): C07F9/6561C07C51/41C07C57/15
Inventor 朱卫兵姚勇周月萍刘俊方冰王显芹孙小虎周琴张荣平王晓军胡红亮
Owner 安徽安科恒益药业有限公司
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