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Stable 5-methyltetrahydrofolate crystal form and preparation method thereof

A technology of methyltetrahydrofolate and methyltetrahydrofolate, which is applied in the field of stable amorphous 5-methyltetrahydrofolate and its preparation, can solve the problem that the temperature control requirements are very strict, the time is long, and the operation Cumbersome and other problems, to achieve the effect of short time, good stability and simple reaction steps

Active Publication Date: 2012-11-14
北京金康和信药业科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Among them, the method for preparing amorphous 5-methyltetrahydrofolate described in patents US2010 / 0168117 and CH699426 is not only cumbersome to operate, but takes a long time, up to 20 hours, and also requires very strict temperature control

Method used

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  • Stable 5-methyltetrahydrofolate crystal form and preparation method thereof
  • Stable 5-methyltetrahydrofolate crystal form and preparation method thereof
  • Stable 5-methyltetrahydrofolate crystal form and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0035] 30ml of deionized water, add 2.10 grams of (6S)-5-MTHF, neutralize with 2mol / L liquid caustic soda under stirring until the pH value is 7.0 to completely dissolve the (6S)-5-MTHF, add 10% calcium chloride solution ( Containing 0.5 grams of calcium chloride), transferred to an ultrasonic reactor with a frequency of 40KHz and a power of 500w, controlled the temperature of the solution at 15°C, ultrasonically reacted for 60 minutes, filtered, and washed. Vacuum-dried at 25° C. to obtain 1.08 g of white amorphous (6S)-5-MTHF calcium salt. The chemical purity is 98.7%.

Embodiment 2

[0037] 30ml of deionized water, add 2.10 grams of (6S)L-5-MTHF, neutralize with 2mol / L ammonia water under stirring until the pH value is 7.0 to completely dissolve the (6S)-5-MTHF, add 10% calcium chloride solution ( Containing 0.5 grams of calcium chloride), transferred to an ultrasonic reactor with a frequency of 40KHz and a power of 800w, controlled the temperature of the solution at 10°C, ultrasonically reacted for 65 minutes, filtered, and washed. Vacuum-dried at 25° C. to obtain 1.10 g of white amorphous (6S)-5-MTHF calcium salt. The chemical purity is 98.6%.

Embodiment 3

[0039] 60ml of deionized water, add 5.05 grams of (6S)-5-MTHF, neutralize with 2mol / L liquid caustic soda under stirring until the pH value is 7.5 to (6S)-5-MTHF is completely dissolved, add 10% calcium chloride solution ( Containing 1.0 grams of calcium chloride), transferred to an ultrasonic reactor with a frequency of 60KHz and a power of 500w, controlled the temperature of the solution at 5°C, ultrasonically reacted for 70 minutes, filtered, and washed. Vacuum drying at 25° C. gave 1.88 g of white amorphous (6S)-5-MTHF calcium salt. Chemical purity 98.5%.

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Abstract

The invention discloses a stable amorphous 5-methyltetrahydrofolate salt and a preparation method of the 5-methyltetrahydrofolate salt; the method comprises the steps of: firstly, neutralizing 5-methyltetrahydrofolate with alkali in aqueous medium until complete dissolution, adding alkaline-earth metal salt or alkaline-earth metal salt solution into the neutralized solution, controlling the temperature of the mixed solution to be within the range of 0-20 DEG C, carrying out ultrasonic treatment, and separating out the amorphous 5-methyltetrahydrofolate salt. The amorphous 5-methyltetrahydrofolate salt has higher stability; and the preparation method is simple in reaction steps, short in time, free from pollution, high in purity, good in stability and more suitable for industrial scale application.

Description

technical field [0001] The invention belongs to the technical field of medicine synthesis, and in particular relates to a stable amorphous 5-methyltetrahydrofolate and a preparation method thereof. Background technique [0002] The chemical name of 5-methyltetrahydrofolate is N-[4-[[(2-amino-1,4,5,6,7,8-hexahydro-4-oxo-5-methyl-6-pterene Pyridyl)methyl]amino]benzoyl]-L-glutamic acid, referred to as 5-MTHF. Structural formula is as shown in formula I: [0003] [0004] Formula I [0005] 5-Methyltetrahydrofolate is the main form of folic acid in tissues and blood, and participates in many important biochemical reactions in the body, such as the biosynthesis of purine and thymine. It does not need to go through cumbersome enzymatic steps in the human body and can be directly utilized. 5-Methyltetrahydrofolate is mainly used as active ingredients of medicines and food additives. It can prevent fetal neural tube defects and arteriosclerosis, treat megaloblastic anemia, an...

Claims

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Application Information

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IPC IPC(8): C07D475/04A61K31/519A61P39/02A61P7/06A61P35/00A61P15/00A61P25/00A61P9/00A61P9/12A61P37/02A23L1/30
Inventor 成永之黄恒
Owner 北京金康和信药业科技有限公司
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