1770840-43-1Relevant articles and documents
Process for synthesizing 7 -iodopyrrolo [2,F] [1,m-triazine -4 - amine
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, (2021/11/21)
The invention belongs to the technical field of chemical synthesis of medicines, and relates to a synthesis process of 7-iodo pyrrolo [2, 1-F] [1, 2, 4] triazine-4-amine. According to the invention, 2, 5-dimethoxy tetrahydrofuran and acethydrazide are used as initial raw materials, and are subjected to substitution, cyanation, deacetylation, cyclization and iodination reactions to obtain 7-iodopyrrolo [2, 1-F] [1, 2, 4] triazine-4-amine. The preparation method is simple, the initial raw materials are 2, 5-dimethoxytetrahydrofuran and acethydrazide which are cheap and easy to obtain. Meanwhile,the yields of the first four steps all reach 85% or above, the productivity is also greatly improved, the total yield of the product is 50% or above, and the purity can reach 99% or above. And meanwhile, the intermediate product is good in quality, so that the dosage of formamidine acetate is reduced when the intermediate IV is prepared. Through experimental comparison, the route has obvious advantages compared with the traditional process route.
Synthesis method of key intermediate 7-halogenated pyrrolo[1,2-F][1,2,4]triazin-4-amine of remdesivir
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, (2021/08/14)
The invention discloses a synthesis method of a key intermediate 7-halogenated pyrrolo[1,2-F][1,2,4]triazin-4-amine of remdesivir as shown in a formula (h). Phthalimide is used as a raw material, and the key intermediate 7-halogenated pyrrolo[1,2-F][1,2,4]triazin-4-amine of remdesivir is synthesized through a series of reactions such as substitution, cyclization, bromination, cyano substitution, hydrazinolysis, heterocyclic ring synthesis and iodination . The post-treatment operation is optimized, and the method has the advantages of being short in reaction time, high in yield, suitable for industrial production and the like.
Synthesis process of retegravir intermediate
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, (2021/03/11)
The invention relates to a synthesis process of a retegravir intermediate 7-iodine-4-amido pyrrolo [2,1-F] [1, 2, 4] triazine. The method comprises the following steps: by using pyrrole as an initialraw material, carrying out aldehyde groupintroduction through phosphorus oxychloride-DMF to obtain 2-aldehyde group pyrrole; preparing a 2-cyano key intermediate through ammonium sulfate, wherein thesteps is the key step of the process; cyclizing the cyano intermediate and formamidine acetate to prepare a 4-amino intermediate; reacting with NIS and adding iodine to prepare the target compound 7-iodine-4-amido pyrrolo [2,1-F] [1, 2, 4] triazine. The whole process has the advantages of simple and easily available raw materials, simple and easy operation, and very high economic value and socialbenefit.