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Preparation method of orlistat

A technology of orlistat and statin, which is applied in the field of orlistat preparation, can solve the problems of expensive and toxic reagents, long preparation steps, and large environmental pollution, and achieve the effects of simple and reasonable design, easy operation, and low environmental pollution

Inactive Publication Date: 2020-08-07
四川奇格曼药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In the route design and method prepared by the prior art, there are disadvantages such as long preparation steps, single strategy, difficult operation of individual reactions, expensive reagents and high toxicity, great environmental pollution and low yield

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Under nitrogen protection, (R,R)-(-)-N,N'-bis(3,5-di-tert-butylsalicylidene)-1,2-cyclohexyldiaminecobalt 6.0g, pentacarbonyl Mix 0.2g of iron alloy, 20g of niborestatin, and 50ml of methanol in a reaction vessel, stir, heat up to 30°C, then add 14g of sodium borohydride, keep the temperature, react for 3 hours, and turn on -5°C to 5°C after the reaction is completed Cool with circulating water, add extractant petroleum ether for extraction, wash twice with dilute hydrochloric acid and water respectively, transfer the organic phase to the distillation pot, distill until there is no fraction, and then use a Roots pump to distill under reduced pressure at -0.098MPa until no liquid drops flow out , to obtain orlistat, the distilled petroleum ether was weighed in barrels, and applied mechanically. Dissolve the obtained orlistat in acetonitrile / petroleum ether mixed solvent (volume ratio 1:25), then heat to 50°C and stir for 15-20 minutes, filter, cool the filtrate, filter wi...

Embodiment 2

[0023] Under the protection of helium, (R,R)-(-)-N,N'-bis(3,5-di-tert-butylsalicylidene)-1,2-cyclohexyldiamine cobalt 10g, pentacarbonyl Mix 0.4g of iron alloy, 20g of niborestatin, and 50ml of ethanol in a reaction vessel, stir, heat up to 33°C, then add 24g of sodium borohydride, keep the temperature, react for 3.5 hours, and turn on -5°C to 5°C after the reaction is completed Circulating water cooling, adding extractant diethyl ether for extraction, washing twice with dilute hydrochloric acid and water respectively, transferring the organic phase to a distillation pot, distilling until there is no fraction, and then distilling under reduced pressure with a Roots pump at -0.098MPa until no liquid drops flow out to obtain Orlistat, the distilled ether was weighed in barrels, and applied mechanically. Dissolve the obtained orlistat in methanol / carbon tetrachloride mixed solvent (volume ratio 1:35), then heat to 54°C and stir for 15-25 minutes, filter, cool the filtrate, suctio...

Embodiment 3

[0025] Under nitrogen protection, (R,R)-(-)-N,N'-bis(3,5-di-tert-butylsalicylidene)-1,2-cyclohexyldiaminecobalt 8g, pentacarbonyl Mix 0.3g of iron, 20g of niborestatin, and 50ml of diethyl ether in a reaction vessel, stir, heat up to 33°C, then add 16g of sodium borohydride, keep the temperature, and react for 4.5 hours. After the reaction, start the cycle at -5°C to 5°C Cool with water, add extractant heptane to extract, wash twice with dilute hydrochloric acid and water, transfer the organic phase to a distillation pot, distill until there is no fraction, and then use a Roots pump to distill under reduced pressure at -0.098MPa until no liquid drops flow out to obtain For orlistat, the distilled heptane was weighed in barrels, and applied mechanically. Dissolve the obtained orlistat in acetonitrile / heptane mixed solvent (volume ratio 1:29), then heat to 58°C and stir for 15-25min, filter, cool the filtrate, suction filter, and vacuum dry to obtain refined orlistat 19.1 g, yi...

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PUM

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Abstract

The invention discloses a preparation method of orlistat. According to the invention, Lipstatin is used as an initial raw material, and cuprous chloride catalyzes reduction reaction of Lipstatin and sodium borohydride to obtain orlistat. The preparation method disclosed by the invention has the advantages of cheap and easily available raw materials, mild process conditions, simple post-treatment,high product yield and few byproducts, and the whole process is very suitable for industrialization.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to a preparation method of orlistat. Background technique [0002] Due to various congenital and acquired factors, obesity patients are becoming more and more, and obesity not only increases the economic burden of human beings, but also causes many diseases, which will indirectly increase the mortality rate. Therefore, it is necessary to find effective and safe Methods to treat obesity, is a hot spot of concern. At present, in the past to treat some severe obese patients, the commonly used drugs include fenfluramine, dexfenfluramine, sibutramine, orlistat, etc., while the drugs fenfluramine or dexfenfluramine Sibutramine is highly toxic and has many side effects, and almost all of it has been discontinued now; although sibutramine is effective, it is a diet inhibitor and is not suitable for long-term use. Orlistat is a commonly used, safe and effective weight loss drug in recen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D305/12
CPCC07D305/12
Inventor 姚静张宪胡伟
Owner 四川奇格曼药业有限公司
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