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Method used for preparing mecobalamin

A technology for methylcobalamin and cyanocobalamin, applied in the field of preparing methylcobalamin, can solve the problems of easy generation of other cobalamin, weak methylation ability, unsuitable for production, etc., and achieves significant economic value and methylation ability. Strong, less toxic effect

Active Publication Date: 2018-02-16
广州普星药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] (1) It is necessary to use methylating reagents. Some methylating reagents have strong toxicity, some have weak methylating ability, are easy to generate other cobalamins, and some are harmful to the environment;
[0008] (2) The purification and refining process requires operations such as column passing, which is inconvenient to operate under dark conditions, and the yield is low, so it is not suitable for production

Method used

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  • Method used for preparing mecobalamin

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Effect test

Embodiment 1

[0049] A method for preparing methylcobalamin, comprising the following steps:

[0050] 1. Reduction reaction: Add 8.0g of cyanocobalamin, 0.3g of cobalt chloride hexahydrate, 6ml of methyl ethyl ketone, and 104ml of water into the flask under the condition of avoiding light, and protect with nitrogen, control the temperature at 30-40°C, stir and dissolve, An aqueous solution of sodium borohydride (3.2 g of sodium borohydride dissolved in 16 ml of water) was slowly added dropwise to the reaction solution at a rate of 4 ml / min. After the addition was complete, the stirring was continued for 30 minutes;

[0051] 2. Methylation reaction: adjust the temperature of the reaction solution to 35-45°C, and immediately add the prepared trimethylsulfoxide iodide solution (2.6g trimethylsulfoxide iodide dissolved in 24ml water) dropwise into the reaction solution , continue stirring for 20 minutes after the dropwise addition;

[0052] 3. Crystallization: Use a mixture of acetone and acet...

Embodiment 2

[0056] A method for preparing methylcobalamin, comprising the following steps:

[0057] 1. Reduction reaction: Add 40.0g of cyanocobalamin, 2.4g of cobalt chloride hexahydrate, 30ml of methyl ethyl ketone, and 500ml of water into the flask under the condition of avoiding light, protect with nitrogen, control the temperature at 30-40°C, and stir to dissolve. An aqueous solution of sodium borohydride (30 g of sodium borohydride dissolved in 300 ml of water) was slowly added dropwise into the reaction solution at a rate of 8 ml / min. After the addition was complete, the stirring was continued for 30 minutes;

[0058] 2. Methylation reaction: adjust the temperature of the reaction solution to 35-45°C, immediately add the prepared trimethylsulfoxide iodide solution (16g trimethylsulfoxide iodide dissolved in 160ml water) dropwise into the reaction solution, Continue stirring for 20 minutes after the dropwise addition;

[0059] 3. Crystallization: Use a mixture of acetone and acetic...

Embodiment 3

[0063] A method for preparing methylcobalamin, comprising the following steps:

[0064] 1. Reduction reaction: Add 20g of cyanocobalamin, 1.0g of cobalt chloride hexahydrate, 16ml of methyl ethyl ketone, and 200ml of water into the flask under the condition of avoiding light. Sodium borohydride aqueous solution (12g of sodium borohydride dissolved in 60ml of water) was slowly added dropwise to the reaction solution at a rate of 6ml / min. After the addition was complete, the stirring was continued for 30 minutes;

[0065] 2. Methylation reaction: adjust the temperature of the reaction solution to 35-45°C, immediately add the prepared trimethylsulfoxide iodide solution (10g trimethylsulfoxide iodide dissolved in 100ml water) dropwise into the reaction solution, Continue stirring for 20 minutes after the dropwise addition;

[0066] 3. Crystallization: Use a mixture of acetone and acetic acid (the volume ratio of acetone and acetic acid is 1:1) to adjust the pH of the reaction sol...

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Abstract

The invention discloses a method used for preparing mecobalamin. The method comprises: dissolving cyanocobalamin, butanone and cobalt chloride hexahydrate in purified water, adding a sodium borohydride solution drop by drop for a reduction reaction, adding trimethylsulfoxonium iodide drop by drop for a methylation reaction to generate mecobalamin, and refining mecobalamin through a crystallizationmethod to obtain high-purity mecobalamin. The provided method is simple and easy, is simple to operate, complete in reaction, mild in condition, high in yield and high in purity, and is particularlysuitable for massive production.

Description

technical field [0001] The invention relates to the technical field of chemical synthesis, in particular to a method for preparing methylcobalamin. Background technique [0002] The English name of methylcobalamin is Mecobalamin, CAS NO: 13422-55-4, the chemical name is: Coα-[α-(5,6)-dimethylbenzimidazolyl]-Coβ-methylcobalamin, and the molecular formula is C 63 h 91 CoN 13 o 14 P, the molecular weight is 1344.40, and the structural formula is as follows: [0003] [0004] Methylcobalamin, also known as methylated vitamin B 12 , as an anti-peripheral neuropathy drug, can directly participate in the metabolism in the body, so it and adenosylcobalamin are both called coenzyme vitamin B 12 Methylcobalamin maintains the stability of cell morphology and function in the body through methylation. It is often used clinically to treat peripheral nerve diseases such as neurological disorders and multiple neuritis caused by diabetes, especially for complications of diabetes suc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H23/00C07H1/00C07H1/06
CPCC07H1/00C07H1/06C07H23/00
Inventor 何演安陈秀秀邓团飞
Owner 广州普星药业有限公司
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