Efavirenz preparation method

A kind of Alphavir and dripping technology, applied in the field of preparation of Alfaviride, can solve the problems of low output, complex manufacturing and high manufacturing cost, and achieve the effects of high output, low cost and simple manufacturing

Inactive Publication Date: 2015-07-01
储海燕
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

Due to the currently prepared efavirenz, the manufacturing cost is high, the manufacturing is complicated, and the yield is low

Method used

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Experimental program
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Embodiment Construction

[0009] Now in conjunction with the present invention for further detailed description.

[0010] A kind of preparation method of efavirem of the present invention, concrete steps are as follows:

[0011] a. Dissolve p-chloroaniline in chloroform and saturated aqueous sodium carbonate solution, add 2,2-dimethylpropionyl chloride dropwise, after the addition is complete, stir at room temperature for 23 hours, collect the solid by filtration, separate the layers of the filtrate, and wash the separated chloroform layer with brine , dried, concentrated;

[0012] b. The residue and the solid obtained above are recrystallized with boiling ethyl acetate-hexane to obtain N-2,2-dimethylpropionyl p-chloroaniline. The acylated product is dissolved in tetrahydrofuran and heated at 0°C Add 2.5mol / L hexane solution of n-butyllithium dropwise, stir for 1h, add ethyl trifluoroacetate dropwise, stir for 30min, add 5% hydrochloric acid and ethyl acetate, separate the organic layer, wash with bri...

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Abstract

The invention relates to an efavirenz preparation method. The method concretely comprises the following steps: 1, washing a separated chloroform layer by using brine, drying, and concentrating; 2, separating out an organic layer, washing the organic layer by using brine, drying, and concentrating to obtain 2-trifluoroacetyl-4-chloroaniline; and 3, adding 1mol / L of hydrochloric acid into n-butanol, reacting at 60DEG C for 72h, and splitting to obtain optically active efavirenz. The efavirenz preparation method has the advantages of simple preparation, high output and low cost.

Description

technical field [0001] The invention relates to the field of drug production, in particular to a preparation method of efavirenz. Background technique [0002] Elfavirex is a non-nucleoside reverse transcriptase inhibitor. It is used in combination with other reverse transcriptase inhibitors for the treatment of HIV-1 infected patients. Due to the currently prepared alfaviride, the manufacturing cost is high, the manufacturing is complicated, and the yield is low. Contents of the invention [0003] The technical problem to be solved by the present invention is: in order to overcome the above-mentioned problems, a preparation method of efavirenz is provided. [0004] The technical scheme that the present invention adopts to solve the technical problem is: a kind of preparation method of alfavire, concrete steps are as follows: [0005] a. Dissolve p-chloroaniline in chloroform and saturated aqueous sodium carbonate solution, add 2,2-dimethylpropionyl chloride dropwise, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D265/18
CPCC07D265/18
Inventor 储海燕
Owner 储海燕
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