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Method for preparing propionyl levocarnitine hydrochloride and application of medicaments thereof

A technology of propionyl-levocarnitine hydrochloride and propionic acid, which is applied in the field of preparation of propionyl-levocarnitine hydrochloride, can solve problems such as difficult operation, and achieve the effects of easy operation, mild conditions and improved efficiency

Inactive Publication Date: 2012-03-28
LEES PHARMA HONG KONG
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  • Summary
  • Abstract
  • Description
  • Claims
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Problems solved by technology

However, the research found that the catalyst in this reaction will cause the racemization of the product PLC, and chiral drugs have high requirements for optical purity, so the products synthesized by this method need to be resolved, which is not easy to operate

Method used

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  • Method for preparing propionyl levocarnitine hydrochloride and application of medicaments thereof
  • Method for preparing propionyl levocarnitine hydrochloride and application of medicaments thereof
  • Method for preparing propionyl levocarnitine hydrochloride and application of medicaments thereof

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preparation example Construction

[0030] The preparation method reaction principle of propionyl L-carnitine hydrochloride of the present invention is as follows:

[0031] Use propionyl chloride to acylate the internal salt of levocarnitine dissolved in propionic acid, add ethyl acetate to crystallize propionyl levocarnitine hydrochloride solution; the suspension is centrifugally dried and purified to obtain propionyl levocarnitine salt salt. The chemical reaction formula is as follows:

[0032]

Embodiment 1

[0035] (1) Preparation of propionic acid solution of internal salt of levocarnitine: use a 3000-liter corrosion-resistant reactor with a constant temperature jacket, such as an enamel reactor, and cover the reaction unit with nitrogen. Add 600kg propionic acid into the reactor, then add 600kg levocarnitine internal salt into the reactor, set the internal temperature of the reactor at T=45°C, keep stirring at a rate of 80rpm, until the suspension is completely dissolved.

[0036] (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 400 kg propionyl chloride and 100 kg propionic acid. The stirring switch of the reactor was turned on to start stirring, and the reactor was cooled to 40° C. through the cooling jacket.

[0037] (3) Acylation reaction: slowly transfer the propionic acid solution of levocarnitine inner salt to the reactor contain...

Embodiment 2

[0043] (1) Preparation of propionic acid solution of internal salt of levocarnitine: use a 3000-liter corrosion-resistant reactor with a constant temperature jacket, such as an enamel reactor, and cover the reaction unit with nitrogen. Add 700kg propionic acid into the reactor, then add 1050kg levocarnitine internal salt into the reactor, set the internal temperature of the reactor at T=42°C, keep stirring at a rate of 80rpm, until the suspension is completely dissolved.

[0044] (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 1400 kg propionyl chloride and 140 kg propionic acid. Turn on the agitation switch of the reactor to start agitation, and cool the reactor to 42°C through the cooling jacket.

[0045] (3) Acylation reaction: slowly transfer the propionic acid solution of levocarnitine inner salt to the reactor containing the ac...

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Abstract

The invention relates to a method for preparing propionyl levocarnitine hydrochloride and application of medicaments thereof. The method comprises the following steps of: (1) mixing and stirring propionic acid and levocarnitine inner salt to prepare propionic acid solution of the levocarnitine inner salt, wherein a mass ratio of the propionic acid to the levocarnitine inner salt is 1:(0.5-1.5); (2) mixing and stirring the propionic acid and propionyl chloride to prepare an acylated reagent, wherein a mass ratio of the propionic acid to the propionyl chloride is 1:(1.5-10); and (3) mixing the propionic acid solution of the levocarnitine inner salt and the acylated reagent, and performing acidylation reaction to obtain the propionyl levocarnitine hydrochloride. The method is mild in condition, safe in reaction, easy to operate and low in cost, and waste gas is not generated. The medicaments which take the propionyl levocarnitine hydrochloride as active ingredients are used for treating peripheral arterial diseases and chronic congestive heart failure to enhance athletic ability, and have a good effect.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a preparation method of propionyl levocarnitine hydrochloride and its medicine application. Background technique [0002] Peripheral arterial disease (PAD) is a chronic ischemic disorder of the extremities resulting from impaired metabolism and function of muscles. The damage process is divided into four phases by Fontain. Stage I manifests as subclinical changes in blood flow. Stage II is characterized by intermittent claudication (IC), where pain forces the patient to stop during periods of higher energy demands such as walking. Patients with stage III PAD have severely reduced blood flow causing pain at rest. In the most severe case (Stage IV), the patient develops nutritional impairment with leg ulcers and / or gangrene. In the United States, 9.6% of cardiovascular events are due to peripheral arterial disease (PAD) presenting as IC. It is directly related to 770,000 hos...

Claims

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Application Information

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IPC IPC(8): C07C229/22C07C227/14A61K31/205A61P9/04A61P9/10
Inventor 李小羿戴向荣张国辉杨中强
Owner LEES PHARMA HONG KONG
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