1-Methyl-1H-[1,2,4]triazole-3-carboxylic acid methyl ester CAS NO.57031-66-0

Methyl 1-methyl-1h-1,2,4-triazole-3-formic acid, CAS: 57031-66-0, English Name: 1-methyl-1h - [1,2,4] triazole-3-carboxylicacidmethylester. Triazole is a heterocyclic compound containing three nitrogen atoms. Its pharmacophore shows a variety of biological activities, such as antifungal, antituberculous, antiviral and so on. Triazole containing compounds have become one of the hot and important fields of drug synthesis research and development in recent years. At present, many antimicrobial drugs containing triazole have been used in clinic and play a variety of roles. 1,2,4-triazole can inhibit the growth of Mycobacterium tuberculosis by blocking lipid biosynthesis or other mechanisms. 1,2,4-triazole not only has antibacterial activity, but also has a variety of biological activities such as anti-tumor, anti HIV, anti influenza, anti-inflammatory, anti malaria, anti hepatitis C and anti tuberculosis, and has the advantages of broad spectrum, high efficiency, low toxicity and low drug resistance. It widely exists in drug molecules, such as antineoplastic drug anastrozole, psychotropic drug triazolam, anti HIV drug melatonin and antifungal drug terconazole.

A preparation method of methyl 1-methyl-1h-1,2,4-triazole-3-formate

technical field

The invention relates to a preparation method of methyl 1-methyl-1h-1,2,4-triazole-3-formate, belonging to the technical field of organic synthesis.

Background technology

Methyl 1-methyl-1h-1,2,4-triazole-3-formic acid, CAS: 57031-66-0, English Name: 1-methyl-1h - [1,2,4] triazole-3-carboxylicacidmethylester. Triazole is a heterocyclic compound containing three nitrogen atoms. Its pharmacophore shows a variety of biological activities, such as antifungal, antituberculous, antiviral and so on. Triazole containing compounds have become one of the hot and important fields of drug synthesis research and development in recent years. At present, many antimicrobial drugs containing triazole have been used in clinic and play a variety of roles. 1,2,4-triazole can inhibit the growth of Mycobacterium tuberculosis by blocking lipid biosynthesis or other mechanisms. 1,2,4-triazole not only has antibacterial activity, but also has a variety of biological activities such as anti-tumor, anti HIV, anti influenza, anti-inflammatory, anti malaria, anti hepatitis C and anti tuberculosis, and has the advantages of broad spectrum, high efficiency, low toxicity and low drug resistance. It widely exists in drug molecules, such as antineoplastic drug anastrozole, psychotropic drug triazolam, anti HIV drug melatonin and antifungal drug terconazole.

Methyl 1h-1,2,4-triazole-3-formate is an important intermediate for the synthesis of broad-spectrum antiviral drug ribavirin. Methyl 1-methyl-1h-1,2,4-triazole-3-formate is a new and scalable method of substituted bicyclic compounds for the treatment or prevention of HBV or HDV infection and related diseases.

[Chemistry and biodiversity,   2017, Vol. 14, # 12, art. No. e1700351] was synthesized by mixing methyl 1h-1,2,4-triazole-3-formate with methyl iodide in tetrahydrofuran and dropping potassium TERT butanol in 52% yield. Due to the high price of methyl 1h-1,2,4-triazole-3-formate raw material, and the volatile, toxic and expensive price of methyl iodide, the dosage is often excessive, which is not conducive to industrial production. The synthetic equation is as follows:

Therefore, it is necessary to deeply study the synthesis process of methyl 1-methyl-1h-1,2,4-triazole-3-formate, so as to provide a better, easy to obtain raw materials, practical and economical reaction route to meet the growing market demand.
 

1. Raw materials are easy to obtain, the price is cheap, and the production cost is relatively low. Avoid using iodomethane, which is highly toxic, volatile and expensive.

2. Diazotization deamination method, using acetonitrile as solvent, can greatly increase the solubility of diazonium salt, prevent solid precipitation, reduce the temperature during deamination, avoid the decomposition of diazonium salt at high temperature and reduce potential safety hazards.

3. The methylation reaction of amino and carboxyl groups by methylating reagent dimethyl carbonate or dimethyl sulfate has high regional selectivity and the separation yield is as high as 75-80%.
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