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Novel production process of tenofovir

A production process and process technology, applied in the new tenofovir production process field, can solve problems such as high cost and complicated operation, and achieve the effects of reducing raw material costs, simplifying process operation, and reducing safety production risks

Inactive Publication Date: 2011-10-19
SUZHOU TENGLONG BIO PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] In order to overcome the shortcomings of complex operation and high cost in the prior art, the present invention provides a production process of tenofovir with simple operation and low production cost

Method used

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  • Novel production process of tenofovir
  • Novel production process of tenofovir
  • Novel production process of tenofovir

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Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0024] 1. Preparation of Intermediate 1

[0025] Add 40 grams of adenine, 0.94 grams of sodium hydroxide and 180 milliliters of N,N-dimethylformamide into a 1000 milliliter four-neck flask equipped with a thermometer, reflux condenser and constant pressure dropping funnel, and maintain the temperature at 25-30 °C and stirred for 10 minutes. At this temperature, 38.2 g of (R)-propylene carbonate were added dropwise. After dropping, the temperature was raised to 120°C, and after refluxing for 22 hours, the system was in a clear state. The temperature was lowered to 70° C., and 240 ml of a 1:1 methanol:isopropanol mixture was added, and a large amount of off-white solid was precipitated. After suction filtration, the filter cake was washed with 40 ml of 1:1 methanol:isopropanol mixture and then vacuum-dried to obtain 37.6 g of the product with a yield of 65.9%.

[0026] 2. Preparation of Intermediate 3

[0027] Add 20 grams of intermediate 1, 100 milliliters of N-methylpyrrol...

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Abstract

The invention relates to a production process of drug tenofovir in the field of aids treatment. The process is a method of using adenine as a raw material, condensing toluenesulfonyloxy dimethyl methyl phosphonate by using an intermediate and then hydrolyzing by using an inorganic acid to finally prepare the tenofovir. The production process of the drug tenofovir, provided by the invention, has the characteristic of improving the hydrolysis activity of the intermediate so that the operation of the process production is largely simplified and the production cost of the tenofovir is largely reduced.

Description

(1) Technical field [0001] The invention relates to a production process of Tenofovir, which is used in the field of AIDS treatment. The process uses adenine as a raw material, condenses an intermediate p-toluenesulfonyloxymethylphosphonic acid dimethyl, and then A method for finally preparing tenofovir by hydrolysis with inorganic acid. The feature of the invention is that the hydrolysis activity of the intermediate is improved, thereby greatly simplifying the production process operation and greatly reducing the production cost of tenofovir. (2) Background technology [0002] In 2009, the United Nations reported that the number of HIV-infected people in China had reached 740,000, and sexual transmission is becoming the main transmission route of AIDS in my country. This is a dangerous signal for the spread of AIDS from high-risk groups to the general population, and the prevention and control work is in a critical period. Tenofovir, as the first nucleotide analog approved...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/38
Inventor 成佳刘洋
Owner SUZHOU TENGLONG BIO PHARMA TECH
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