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Preparation method of 5'-nucleotide

A nucleotide and nucleoside technology, applied in the field of nucleoside phosphorylation, can solve the problems of limited scope of substrate action and large screening workload, and achieve the effects of less side reactions, easy purification, and fewer by-products

Active Publication Date: 2012-05-16
STAR LAKE BIOSCI CO INC ZHAOQING GUANGDONG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage of this method is that the workload of enzyme screening is very large, and the scope of enzyme substrate action is also limited.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Put 100g of inosine into a 500ml three-necked bottle, add 1400g of triethyl phosphate, stir, add 0.5g of tetrazole and 0.5g of m-chloroperoxybenzoic acid, cool down to -10°C, slowly add 130g of phosphorus oxychloride, 3 Hours later, a sample was taken for detection, and the peak retention time of the target product in high performance liquid chromatography was consistent with the retention time of the 5'-inosinic acid standard product, and the yield of 5'-inosinic acid was calculated according to the high performance liquid chromatography method to be 97.2%.

Embodiment 2

[0022] Put 100g of guanosine into a 500ml three-necked bottle, add 1500g of triethyl phosphate, stir, add 0.5g of tetrazole and 0.5g of m-chloroperoxybenzoic acid, cool down to -10°C, slowly add 140g of phosphorus oxychloride, 3 Hours later, a sample was taken for detection, and the peak retention time of the target product in high performance liquid chromatography was consistent with the retention time of the 5'-guanylic acid standard product, and the yield of 5'-guanylic acid was calculated according to the high performance liquid chromatography method to be 96.8%.

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PUM

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Abstract

The invention discloses a preparation method of 5'-nucleotide, comprising the following steps of: suspending nucleoside in an organic solvent containing tricresyl phosphate low-level alkyl ester; adding a catalyst; and then contacting an obtained suspension with a phosphorylation reagent at the temperature of -30-20 DEG C so that the nucleoside is phosphorylated to obtain the 5'-nucleotide, wherein the weight ratio of the nucleotide and the catalyst is 100:0.5-1.5. The method can be used for preparing the high-purity high-yield 5'-nucleotide, shortens the time of the phosphonation reaction ofthe nucleotide, is easier to eliminate the impurities during the purification of the nucleoside and reduces the difficulty of post process.

Description

technical field [0001] The invention relates to a nucleoside phosphorylation method, in particular adding a catalyst to a suspension reaction solution to improve the phosphorylation selectivity of the 5'-position hydroxyl of the nucleoside and suppress the formation of by-products. Background technique [0002] Nucleotides have a wide range of uses in the agriculture, food and pharmaceutical industries. Especially in the application of baby food and medicine, it has an irreplaceable function. In the field of medicine, clinical experiments have shown that nucleotides participate in human metabolism, promote the improvement and recovery of internal organs, improve the hematopoietic function of bone marrow, and can be used as an auxiliary drug for the treatment of cancer viruses. It is a very important pharmaceutical raw material. In addition to the application in the pharmaceutical industry, nucleic acid substances also play an important role in the fine chemical and food ind...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H1/02C07H19/20
Inventor 任洪发林晓王海波鲁立王晓明欧仁树黄桂基宁异真
Owner STAR LAKE BIOSCI CO INC ZHAOQING GUANGDONG