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Preparation method of acetyl levocarnitine hydrochloride, and drug application of acetyl levocarnitine hydrochloride

A technology of levocarnitine base and hydrochloride, which is applied in the field of preparation of acetyl levocarnitine hydrochloride, can solve the problems of affecting the quality of recrystallization products, large consumption of glacial acetic acid, long heating time, etc. Low, reaction-safe, and easy-to-handle effects

Inactive Publication Date: 2012-05-02
LEES PHARMA HONG KONG
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are three disadvantages in this method: the consumption of glacial acetic acid is large, and the cost is high; crystallization needs to depressurize and recover excess acetyl chloride and glacial acetic acid first, and because of the long heating time, side reactions are easy to occur, such as: elimination reaction occurs to generate croton betaine ; Anhydrous isopropanol is used as a solvent for recrystallization, and the solubility is low, which affects the quality of recrystallization products
The use of catalysts in this method is likely to cause racemization of the product, and chiral drugs have high requirements for optical purity and are not easy to operate

Method used

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  • Preparation method of acetyl levocarnitine hydrochloride, and drug application of acetyl levocarnitine hydrochloride
  • Preparation method of acetyl levocarnitine hydrochloride, and drug application of acetyl levocarnitine hydrochloride
  • Preparation method of acetyl levocarnitine hydrochloride, and drug application of acetyl levocarnitine hydrochloride

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preparation example Construction

[0028] The preparation method reaction principle of acetyl-levocarnitine hydrochloride of the present invention is as follows:

[0029] Use acetyl chloride to acylate the internal salt of levocarnitine dissolved in acetic acid, add ethyl acetate, acetyl levocarnitine hydrochloride crystallizes out from the solution, and obtain purified acetyl levocarnitine after centrifugal drying Hydrochloride. The chemical reaction formula is as follows:

[0030]

Embodiment 1

[0033] (1) Preparation of acetic acid solution of levocarnitine base: adopt a 3000-liter corrosion-resistant reactor with a constant temperature jacket, such as an enamel reactor, and cover the reaction unit with nitrogen. Add 800kg acetic acid in the reactor, then add 960kg levocarnitine base in the reactor, start to stir the reactor. The temperature inside the reactor was set at 40° C., and the suspension was maintained until it was completely dissolved.

[0034] (2) Preparation of acylating reagent: use a 6000-liter corrosion-resistant reactor with a constant temperature jacket, such as an enamel reactor, and cover the reaction unit with nitrogen. Add 600 kg of acetyl chloride and 200 kg of hydrochloric acid, start stirring, and cool the reactor to below 30° C. through the cooling jacket.

[0035] (3) Acylation reaction: slowly transfer the acetic acid solution of levocarnitine base to the reactor containing the acylating reagent. Due to the exothermic reaction, the tempe...

Embodiment 2

[0041] (1) Preparation of acetic acid solution of levocarnitine base: adopt a 2500-liter corrosion-resistant reactor with a constant temperature jacket, such as an enamel reactor, and cover the reaction unit with nitrogen. Add 600kg acetic acid in the reactor, then add 540kg levocarnitine base in the reactor, start to stir the reactor. The internal temperature of the reactor was set at 42° C., and the suspension was maintained until it was completely dissolved.

[0042] (2) Preparation of acylating reagent: use a 5000-liter corrosion-resistant reactor with a constant temperature jacket, such as an enamel reactor, and cover the reaction unit with nitrogen. 300 kg of acetyl chloride and 150 kg of hydrochloric acid were added, stirring was started, and the reactor was cooled to below 30° C. through the cooling jacket.

[0043] (3) Acylation reaction: slowly transfer the acetic acid solution of levocarnitine base to the reactor containing the acylating reagent. Due to the exothe...

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Abstract

The invention relates to a preparation method of acetyl levocarnitine hydrochloride, and drug application of the acetyl levocarnitine hydrochloride. The preparation method comprises the following steps of: (1) mixing acetic acid and levocarnitine base, and then stirring to prepare an acetic acid solution of the levocarnitine base, wherein the mass ratio of the acetic acid to the levocarnitine base is 1: 0.6 to 1.2; (2) mixing hydrochloric acid and acetyl chloride, and then stirring to prepare an acylation reagent, wherein the mass ratio of the hydrochloric acid to the acetyl chloride is 1: 2 to 4; and (3) mixing the acetic acid solution of the levocarnitine base and the acylation reagent, and performing acylation reaction to prepare the acetyl levocarnitine hydrochloride. The method is easy to operate and low in cost. Waste gas can be avoided. Drugs with the acetyl levocarnitine hydrochloride as an active ingredient are used for treating mechanical and inflammatory damages of peripheral nerve trunks or nerve roots with good effect.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a preparation method of acetyl-levocarnitine hydrochloride and its medicine use. Background technique [0002] There are many types of peripheral neuropathy, which are generally characterized by sensory and motor dysfunction of one or more nerve trunks. There are many causes of peripheral neuropathy, including diabetic peripheral neuropathy, peripheral neuropathy caused by neurotoxicity of chemotherapy drugs, and peripheral neuropathy caused by HIV infection. [0003] Diabetic peripheral neuropathy is a variety of neurological diseases caused by diabetes, and it is the most common type of chronic complications of diabetes. Diabetics have long-term high blood sugar, which leads to the degeneration of the nervous system, and the local hypoxia caused by diabetic microangiopathy, which eventually leads to the destruction of nerve cells and nerve fibers, and corresponding symptoms ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C229/22C07C227/30C07C227/18A61K31/221A61P25/00A61P25/02
Inventor 李小羿戴向荣张国辉杨中强
Owner LEES PHARMA HONG KONG
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