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A new process for the preparation of tenofovir by "one pot method"

A new process and suitable technology, applied in the field of tenofovir synthesis, can solve the problems of rising production cost and reducing production efficiency, and achieve the effect of improving production efficiency, easy to scale up, and reducing production cost

Active Publication Date: 2017-01-11
成都伊诺达博医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Complicated post-processing will inevitably lead to a reduction in production efficiency
All of the above will lead to an increase in production costs

Method used

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  • A new process for the preparation of tenofovir by "one pot method"
  • A new process for the preparation of tenofovir by "one pot method"
  • A new process for the preparation of tenofovir by "one pot method"

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Experimental program
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Embodiment Construction

[0029] The purpose of the present invention is to invent a method for synthesizing tenofovir (PMPA) with simple technique, strong operability, high yield and lower cost.

[0030] Specifically, the present invention provides a new process for synthesizing tenofovir (PMPA).

[0031] A major feature of the present invention is to use adenine (compound I) as a raw material to prepare PMPA (compound V) through a "one-pot method". When preparing compound II and compound IV, the reaction liquid can be directly put into the next reaction without undergoing complex post-treatments such as distillation, drying, filtration, and purification, which greatly simplifies the operation process. The present invention only uses one organic solvent from the beginning to the end, avoiding the use and recovery of multiple solvents and the generation of various waste water and waste gas. These all greatly reduce the production cost of Tenofovir (PMPA).

[0032] Specifically, the involved key synth...

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Abstract

The present invention discloses a new process for preparing tenofovir through a one-pot method. According to the present invention, the traditional three-step complex operation is discarded and is simplified into the one-pot method operation, such that the complex post-treatment operation in the middle link is avoided, and the production efficiency is substantially improved; and the new process has characteristics of simple step, mild conditions, easy operation, and easy scale-up, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical synthesis technology, in particular to a synthesis method of Tenofovir. Background technique [0002] Tenofovir disoproxil fumarate (TDF), the chemical name is (R)-[[2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methanol Base] phosphonic acid diisopropoxycarbonyloxy methyl ester fumarate, its structure is shown in formula (VI), is researched and developed by U.S. Glead Sciences company, listed in the U.S. for the first time in October, 2001, now in Europe, Listed in countries and regions such as Australia and Canada. At the 58th American Association for the Study of Liver Diseases Annual Meeting in November 2007 and the 43rd European Liver Diseases Annual Meeting in April 2008, reports on the treatment of CHB with tenofovir dipivoxil attracted widespread attention. [0003] Tenofovir disoproxil fumarate is a novel nucleoside (acid) analogue approved by the US Food and Drug Administration (FDA)...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F9/6561
Inventor 付清泉岳利剑周平斯涛赵茂先张银
Owner 成都伊诺达博医药科技有限公司