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Method for separating non-geometric proportion cis-sertraline hydrochloride mixture

A technology of sertraline hydrochloride and separation method, which is applied in the field of separation of proportional cis-sertraline hydrochloride mixture, can solve the problems of polluting the environment, not being effectively used, wasting resources, etc.

Inactive Publication Date: 2008-01-09
ZHEJIANG LEPU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] In Example 2 of the patent US4536518, the free resolution of cis-sertraline racemate hydrochloride was carried out to obtain sertraline mandelate, and its yield was only 41.2% by calculation, indicating that there were still Containing 14.97% of cis-(+) sertraline has not been effectively utilized, and expensive materials are discarded in vain, which not only wastes resources, but also seriously pollutes the environment

Method used

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  • Method for separating non-geometric proportion cis-sertraline hydrochloride mixture

Examples

Experimental program
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Effect test

Embodiment 1

[0016] With 50kg cis-sertraline hydrochloride mixture (cis-(+) sertraline hydrochloride: cis-(-) sertraline hydrochloride=15:85) and 250L methanol aqueous solution (the quality of water Percentage is 3%) drop in the reaction pot of 500L, stir and heat to 40 ℃ of insulation 10 hours, under this temperature, filter while hot, filter cake is dried, obtain cis-racemate sertraline hydrochloride 14kg; Filtrate The temperature was lowered to crystallize, filtered and dried to obtain 32.5 kg of cis-(-)sertraline hydrochloride.

Embodiment 2

[0018] 50kg cis-sertraline hydrochloride mixture (cis-(+) sertraline hydrochloride: cis-(-) sertraline hydrochloride=10:90) and 300L n-propanol aqueous solution (water The mass percentage is 15%) into a 500L reaction pot, stirred and heated to 60 ° C for 8 hours, at this temperature, filtered while hot, and the filter cake was dried to obtain cis-racemate sertraline hydrochloride 9.6 kg; the filtrate cooled and crystallized, filtered and dried to obtain cis-(-) sertraline hydrochloride 36.7kg.

Embodiment 3

[0020] 50kg cis-sertraline hydrochloride mixture (cis-(+) sertraline hydrochloride: cis-(-) sertraline hydrochloride=5:95) and 150L ethanol and isopropanol ( Volume ratio 50:50) aqueous solution (mass percentage of water is 12%) is put into the reaction pot of 500L, stirring and heating to 50 ℃ for 16 hours, at this temperature, filter while hot, filter cake is dried, obtains cis 4.4 kg of rotamer sertraline hydrochloride; the filtrate cooled to crystallize, filtered and dried to obtain 42.4 kg of cis-(-) sertraline hydrochloride.

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PUM

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Abstract

A method for separating cis-Schtrilin hydrochloride mixture is carried out by keeping temperature for mixture of cis-(+) Schtrilin hydrochloride and cis-(-) Schtrilin hydrochloride in solution of methanol, ethanol, 2-propanol, 1-propanol or their mixtures at a range of 40 deg. C to solvent reflux temperature, agitating for 1-16 hrs, filtering, separating to obtain cis-racemic Schtrilin hydrochloride, decreasing temperature and crystallizing to obtain final product. It's simple and safe and has full use of resources.

Description

technical field [0001] The invention relates to a method for separating a cis-sertraline hydrochloride mixture, in particular to a method for separating a non-equal ratio cis-sertraline hydrochloride mixture. Background technique [0002] The cis-sertraline hydrochloride mixture contains pharmaceutically active ingredients suitable for its antidepressant properties. Sertraline hydrochloride: (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthylamine hydrochloride, has the following Formula structure: [0003] [0004] Sertraline hydrochloride [0005] In the patent US4536518, it is disclosed to synthesize sertraline-1-imine from sertrane (sertralone), and then obtain cis-sertraline hydrochloride racemate through reduction and separation, and then to cis-sertraline salt The salt racemate is freed, separated and refined by D-(-)mandelic acid to obtain sertraline mandelate, and finally the sertraline mandelate is freed and salified with hydrochloric acid ...

Claims

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Application Information

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IPC IPC(8): C07C211/42C07C209/88
Inventor 沈如恩陶激扬万永明陈志荣王云德洪华斌
Owner ZHEJIANG LEPU PHARMA CO LTD
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