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CAS NO.148553-50-8
High(1-50)KilogramHigh(51-500)Kilogram
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Export High Quality Pregabalin 148553-50-8 For Sale
Quick Details
Classification: Pharmaceutical Intermediates
Cas NO.: 148553-50-8
Name: Pregabalin
Formula: C8H17NO2
Melting Point: 194-196ºC
Boiling Point: 274.0±23.0 °C at 760 mmHg
Refractive index: 1.465
Flash Point: 119.5±22.6 °C
Density: 1.0±0.1 g/cm3
PSA: 63.32000
LogP: 1.12
Adverse effects: Pregabalin can be associated with adverse effects at the level of the nervous system and other systems.
Clinical Use:Antiepileptic,,Neuropathic pain ,Generalised anxiety disorder
Usage: Pregabalin has an approved indication and is widely used for the treatment of generalized anxiety disorder. Several randomized, double- blind, placebocontrolled trials found that pregabalin is an effective treatment for patients with generalized anxiety disorder and social anxiety disorder. Possible implications in the treatment of mood disorders and benzodiazepines dependence are emerging. Moreover, pregabalin may be a therapeutic agent for the treatment of alcohol abuse, in both withdrawal phase and relapse prevention.
The contents of the invention
In order to overcome the shortcomings of the prior art, it is an object of the present invention to provide a preparation method of pregabalin which is simple in process and effective in impurity control and is suitable for large-scale industrial production.
A method for the preparation of pregabalin, comprising the steps of:
(1)(R) - (-) - 3-carbamoylmethyl-5-methylhexanoic acid and sodium hypochlorite aqueous solution in an aqueous sodium hydroxide solution to give the reaction solution I;
(2)After the reaction solution I is cooled, the reducing agent is added and the sodium hypochlorite is destroyed, and the reaction liquid II is heated to obtain the reaction liquid II;
(3)The reaction liquid II is added with a catalyst, and hydrogen is added to carry out the reduction reaction, and the filtrate I is obtained by filtration;
(4)Filtrate I by adding concentrated hydrochloric acid, by stirring, filtration, solid wet goods;
(5)Solid wet product added to the isopropyl alcohol and water, stirring and stirring, filter, the filtrate by cooling, stirring, filtration, filter cake was dried after the Puri Bahrain.
In the above preparation route, the specific process conditions of each step are as follows:
(A) in step (1):
The mass fraction of sodium hydroxide aqueous solution is related to the quality and yield of the product, reducing the mass fraction of the aqueous solution of sodium hydroxide, facilitating the dissolution of the inorganic salt, improving the quality of the product and improving the mass fraction of the aqueous solution of sodium hydroxide. The yield of the sodium hydroxide aqueous solution is preferably 20 to 35% by weight,
Wherein the mass fraction of the aqueous sodium hypochlorite solution is from 5 to 15%, and the mass fraction of the sodium hypochlorite aqueous solution is 9 to 15%, and the aqueous sodium hypochlorite solution is added dropwise to the (R) - (-) - 3- Carbamylmethyl-5-methylhexanoic acid and sodium hydroxide aqueous solution, it is advantageous to reduce the generation of impurities by adding an aqueous solution of sodium hypochlorite in a dropping manner because the reaction is an exothermic reaction;
(R) - (-) - 3-carbamoylmethyl-5-methylhexanoic acid, the molar ratio of sodium hypochlorite to sodium hydroxide is 1: 0.8 to 1.3: 2 to 3, the sodium hypochlorite And the yield of pregabalin is closely related, and the dosage of sodium hydroxide will affect the purity of the product, in this ratio, can effectively reduce the impurities, and the higher yield;
Packaging & Delivery
Packaging Detail: customized
Payment Term: T/T or L/C, D/P, DIA, WU, MG
Delivery Detail: Usually within 3-5 working days after full payment Shipping: EMS, DHL, TNT, UPS, FEDEX, BY AIR, BY SEA
Our Company
Hebei Youze Biological Technology Co., Ltd. has a registered capital of 1 million yuan and is one of the most dynamic foreign trade companies in the Chinese market. We have a pharmaceutical raw material production plant and a reagent R&D center. We now have the most complete product line. In addition, we have developed and produced tens of thousands of reagents. We also have the business of custom synthesis of various organic compounds as a supplement. We can synthesize almost all chemicals. Our goal is to survive by quality and develop by credit.
In the past two years, our products have spread over more than 30 countries in the world, Europe, South America, North America, Southeast Asia and Africa. We work with friends all over the world to develop the best quality products, the most reasonable prices and safe and effective transportation. Product can be ordered from milligrams to tons. Meet the purchase of new and old customers. We will not let you down.