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Preparation method of lurasidone hydrochloride

A technology for lurasidone hydrochloride and hydrochloric acid solution, which is applied in organic chemistry and other fields, and can solve problems such as insoluble, product loss, and increased manufacturing costs

Pending Publication Date: 2021-06-25
SHANGHAI SYNCORES TECH INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, according to the above-mentioned patent description, when using hydrochloric acid with a concentration of 1.8% for the salt-forming reaction, the yield of the obtained compound is only 65%, and a large amount of product is lost in the mother liquor
It can be seen that when the above process is applied to mass production, it will cause an increase in manufacturing costs.
[0007] In addition, we tried to form a salt in an alcoholic solvent, and found that the free base of lurasidone was insoluble in an alcoholic solvent. Under reflux conditions, an alcoholic solvent that was more than 20 times the mass of the free base was required to be fully soluble. When mass production, there are great limitations

Method used

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  • Preparation method of lurasidone hydrochloride
  • Preparation method of lurasidone hydrochloride
  • Preparation method of lurasidone hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] 10g of lurasidone free base (compound II), was added to the mixed system of 80mL ethanol and 20mL dichloromethane, the system was warmed up to reflux and dissolved, and then the premixed hydrochloric acid ethanol solution (2.26g 36% concentrated hydrochloric acid+ 20mL ethanol), after the dropwise addition, keep warm and reflux and stir for 1-2h, the system is turbid; start to cool down, within 2-3h, the system slowly cools down to 0-10°C, keep warm at 0-10°C, stir for 1-2h; filter, filter The cake was dried under vacuum at 45-50° C. to obtain 10.5 g of lurasidone hydrochloride (compound I), with a yield of 98%, residual ethanol: 11 ppm, and residual dichloromethane: 39 ppm.

Embodiment 2

[0026] 10g of lurasidone free base (compound II), was added to the mixed system of 90mL ethanol and 20mL dichloromethane, the system was warmed up to reflux and dissolved, and then the premixed hydrochloric acid ethanol solution (6.17g 36% concentrated hydrochloric acid+ 10mL ethanol), after the dropwise addition, keep warm and reflux and stir for 1-2h, the system is turbid; start to cool down, within 2-3h, the system slowly cools down to 0-10°C, keep warm at 0-10°C, stir for 1-2h; filter, filter The cake was dried under vacuum at 45-50° C. to obtain 10.5 g of lurasidone hydrochloride (compound I), with a yield of 98%, residual ethanol: 6 ppm, residual dichloromethane: 43 ppm.

Embodiment 3

[0028] Add 50g of lurasidone free base (compound II) into the mixed system of 500mL of ethanol and 50mL of dichloromethane, heat up the system to reflux and dissolve, then add 11.31g of 36% concentrated hydrochloric acid while keeping warm, after the addition is completed, keep stirring under reflux for 1~ 2h, the system was turbid; began to cool down, within 2-3h, the system slowly cooled down to 0-10°C, kept at 0-10°C, stirred for 1-2h; filtered, and the filter cake was vacuum-baked at 45-50°C to obtain 51.53g Lurasidone hydrochloride (compound I), yield 96%, residual ethanol: 19 ppm, residual dichloromethane: 6 ppm.

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Abstract

The invention provides a preparation method of lurasidone hydrochloride. The method comprises the step of reacting lurasidone free alkali with hydrochloric acid in a mixed solvent of an alcohol solvent and a haloalkane solvent to obtain the lurasidone hydrochloride. The method provided by the invention has the advantages of high yield, low cost, high safety and low residual solvent content, and is very suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a method for preparing lurasidone free base and its hydrochloride. [0002] technical background [0003] Lurasidone hydrochloride jointly developed by Dainippon Sumitomo and Sunovion is a dopamine and serotonin receptor inhibitor for the treatment of schizophrenia and bipolar disorder. Lurasidone hydrochloride is expected to be a more effective and safer drug because it can reduce extrapyramidal reactions and cardiac side effects and control weight gain. On October 28, 2010, the U.S. Food and Drug Administration (FDA) approved its marketing, with a trade name of Latuda, for the treatment of schizophrenia. Canada has also been approved. [0004] Lurasidone hydrochloride is an atypical antipsychotic drug. The exact mechanism of its treatment of schizophrenia is still not very clear like other atypical antipsychotic drugs. related to antagonism. It is use...

Claims

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Application Information

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IPC IPC(8): C07D417/12
CPCC07D417/12C07D487/10C07D417/08
Inventor 张一凯黄钧正卢浩郭效文姜亚飞高渊海黄鲁宁陶安平安建国顾虹
Owner SHANGHAI SYNCORES TECH INC
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