Exemestane synthesis technology

A technology of exemestane and a synthesis process, applied in the field of exemestane synthesis technology, can solve the problems of low production efficiency, complex production process, low separation efficiency, etc., achieves improved utilization, overcomes many processes, and improves The effect of work efficiency

Inactive Publication Date: 2016-06-01
赵建英
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the current synthesis process of exemestane, the process flow is not easy to implement, the separation efficiency is low, the recycling of raw materials cannot be realized, the production process is complicated, and the production efficiency is low

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0011] The synthetic technique of the exemestane of the present embodiment comprises the following steps:

[0012] (1) The synthesis of 6-methylene-androst-4-ene 3,17-dione includes the following steps: A. androstenedione, tetrahydrofuran, absolute ethanol, triethyl orthoformate, p-toluenesulfonic acid Add to the reactor one by one, stir and react at 45°C for 1 hour, then add p-toluenesulfonic acid, and react for 1 hour; B. Add N-methylaniline and 37% formaldehyde, and maintain this temperature for 2 hours, cool to below 20°C, Add concentrated hydrochloric acid dropwise, after the addition, continue to react for 1 hour, cool to 5°C; C. add water, stir and react for 1 hour, filter with suction, wash with water, and dry to obtain 6-methylene-androst-4 in the form of yellow solid -ene 3,17-dione;

[0013] (2) The synthesis of exemestane includes the following steps: A. heating 6-methylene-androst-4-ene 3,17-dione, toluene, and nitrobenzoic acid to reflux; B. adding in batches D...

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PUM

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Abstract

The invention discloses an exemestane synthesis technology. The technology comprises the steps of 6-methylene-androst-4-en-3,17-dione synthesis, crude exemestane synthesis and purification. The technology has the advantages of simple route, easily available raw materials, high yield, and suitableness for domestic industrial production.

Description

technical field [0001] The invention belongs to the field of chemical and pharmaceutical technology, and in particular relates to a synthesis technology of exemestane. Background technique [0002] Exemestane English name Exemestane, chemical name 1,4-diene-3,17-dione-6-methyleneandrostane or 6-methyleneandrostane-1,4-diene-3,17 - Diketones. In the current synthesis process of exemestane, the process flow is not easy to implement, the separation efficiency is low, the recycling of raw materials cannot be realized, the production process is complicated, and the production efficiency is low. Contents of the invention [0003] In order to overcome the above-mentioned technical problems existing in the prior art, the object of the present invention is to provide a synthesis process of exemestane. The present invention not only has a simple production process, improves work efficiency, but also realizes product quality assurance. [0004] The synthetic technique of exemes...

Claims

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Application Information

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IPC IPC(8): C07J1/00
Inventor 赵建英
Owner 赵建英
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