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Synthesis process of weight-reducing drug lorcaserin hydrochloride intermediate

A technology of chlorcaserin hydrochloride and synthesis process, which is applied in the directions of drug combination, active ingredients of heterocyclic compounds, metabolic diseases, etc., can solve the problems of high reaction temperature, many impurities, long time, etc., and achieves the simple operation of the synthesis process and the synthesis of The effect of simple route and low production cost

Pending Publication Date: 2020-04-03
江西博雅欣和制药有限公司
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  • Abstract
  • Description
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  • Application Information

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Problems solved by technology

Although the reaction route is short, the 2-chloropropionyl chloride and borane used are more expensive, and the latter is inconvenient to operate
The high reaction temperature of 150°C and long time for the ring-closing reaction will result in many impurities and difficult separation and purification; a large amount of tetrahydrofuran and other ether solvents are used in the third step reaction, which is expensive, flammable and explosive, And it is not conducive to recycling

Method used

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  • Synthesis process of weight-reducing drug lorcaserin hydrochloride intermediate
  • Synthesis process of weight-reducing drug lorcaserin hydrochloride intermediate
  • Synthesis process of weight-reducing drug lorcaserin hydrochloride intermediate

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Embodiment Construction

[0071] The technical solutions of the present invention will be described in detail below in conjunction with specific embodiments.

[0072] Step 1: Acetylation

[0073] Add 7.4kg of acetic anhydride to the 50L reaction kettle successively, then add 7.5kg of p-chlorophenethylamine dropwise, start stirring and heating, raise the temperature to 50-60°C for 2 hours, take samples and send them to the central control of HPLC; Excess acetic anhydride and by-product acetic acid were removed; 20kg of toluene and water were added for washing, and the organic phase directly entered the next step of allyl substitution reaction after standing for separation.

[0074] Step Two: Replace

[0075] Add 3.0kg of tetrabutylammonium bromide, 11.4kg of allyl bromide, 19.6kg of potassium carbonate and 26.5kg of potassium hydroxide into a 100L reactor, start stirring and raise the temperature to 50°C to 60°C for 10 to 12 hours; filter , the filter cake was washed with a small amount of toluene; th...

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Abstract

The invention discloses a synthesis process of a weight-reducing drug lorcaserin hydrochloride intermediate (compound V), which is characterized in that p-chlorophenylethylamine is used as a raw material, acetic anhydride is subjected to acylation to protect amino, and allyl substitution, Friedel-Crafts alkylation and hydrochloric acid deprotection are performed to obtain a lorcaserin hydrochloride racemate. The synthesis method is simple in synthesis and preparation and high in yield, and is a lorcaserin hydrochloride intermediate synthesis process suitable for industrial large-scale production.

Description

technical field [0001] The invention relates to a new synthesis process of a weight-loss medicine greencaserin hydrochloride intermediate, which belongs to the technical field of drug synthesis. Background technique [0002] Obesity is a multifactorial chronic metabolic disease in which the human body eats more calories than it consumes, and the excess calories are stored in the body in the form of fat. A large body of relevant evidence shows that when the body stores too much energy in the form of fat, that is, beyond normal physiological needs, it can have adverse effects on lifespan and health. As we grow older, body fat increases accordingly, which will increase the risk of cardiovascular disease, affect the endocrine and digestive system, and increase the probability of cancer. [0003] The World Health Organization listed obesity as a disease in 1997, which is one of the four major medical and social problems in the world. Since the 1980s, with the rapid development ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D223/14A61K31/55A61P3/04
CPCC07D223/14A61K31/55A61P3/04
Inventor 王建邓斐冷志
Owner 江西博雅欣和制药有限公司
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