Synthesizing method of weight loss drug orlistat intermediate

A technology of orlistat and a synthetic method, which is applied in the field of synthesis of key intermediates of weight-loss drugs, can solve problems such as long routes and expensive synthesis costs, and achieve the effects of simple operation process, simple operation, and reduced production costs

Active Publication Date: 2018-09-04
DONGGUAN UNIV OF TECH
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Problems solved by technology

[0005] The purpose of the present invention is to overcome the problems of long routes and expensive synthesis costs in the existing synthetic methods, and to provide a new synthetic method for weight-loss drug orlistat intermediates

Method used

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  • Synthesizing method of weight loss drug orlistat intermediate

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Embodiment 1

[0018]1. Synthesis of compound (3): Dissolve Evans (Evans) chiral auxiliary (5.0g, 19.9mmol, 1.0eq) in dichloromethane (60mL) at -78°C and under the protection of nitrogen , slowly added titanium tetrachloride (4.37mL, 39.8mmol, 1.8eq) dropwise to the mixed solution, the solution turned yellow after the addition, and after stirring for 5 minutes, slowly added N, N -Diisopropylethylamine (6.93mL, 2.09mmol, 1.8eq), once added to the reaction system, the solution quickly turns dark red, after the dropwise addition at -78°C, continue to stir at this temperature for 1 hour, Then, the raw material n-dodecaldehyde (2) (4.40g, 23.88mmol, 1.2eq) was dissolved in dichloromethane (20mL), and then this solution was slowly injected into the above reaction system, reacted for 2 hours, and detected by TLC After finding that Evans (Evans) chiral auxiliary agent has reacted, add saturated ammonium chloride solution (20mL) to the mixing system and quench the reaction system, then extract with d...

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Abstract

The invention discloses a method for synthesizing weight loss drug orlistat key intermediate. According to the method disclosed by the invention, n-dodecanal is utilized as a beginning raw material, orlistat intermediate compound (9) is prepared through multiple steps of reaction, and finally, orlistat can be prepared through two steps of known reaction of chiral hydroxyl deprotection reaction andmistsunobu reaction. A synthesizing strategy of the method disclosed by the invention is a typical linear strategy, a route design is simple and reasonable, an operation technology is convenient, reaction conditions are moderate, steps are few, a product yield is high, production cost is remarkably reduced, and the method is suitable for industrial preparation.

Description

technical field [0001] The invention relates to a method for synthesizing a key intermediate of a weight-loss drug, in particular to a method for synthesizing an intermediate of a weight-loss drug orlistat. Background technique [0002] Due to various innate 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, and then indirectly increases the mortality rate, so looking for effective Safe approaches to treating obesity are a hot topic of concern. At present, people usually divide weight-loss drugs into two categories: one is to promote the body’s decomposition and consumption of fat, so as to achieve the purpose of weight loss, such as ephedrine, theophylline, caffeine, and β3-adrenoceptor agonists. etc., they can promote fat metabolism, thereby increasing energy consumption, thereby reducing fat accumulation. Among them, methylxanthines (methylxanthines) and as...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D305/12
CPCC07D305/12
Inventor 王晓季庞易英王继武周毅孙永丽彭莹王博欧文涛肖和盛黄双平
Owner DONGGUAN UNIV OF TECH
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