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 remdesivir intermediate triazinamine derivative
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, (2021/04/10)
The invention discloses a synthesis method of a remdesivir intermediate triazinamine derivative. The remdesivir intermediate triazinamine derivative is prepared by adopting a unique synthesis method. The invention solves the problems of expensive raw materials, large amount of wastewater in the production process and the like in existing reaction of a remdesivir intermediate triazinamine derivative, and provides the novel synthesis method of the remdesivir intermediate triazinamine derivative, wherein the synthesis method has the advantages of simple preparation method, cheap and easily available raw materials, greatly reduced production cost, less wastewater and the like; the synthesis method is never reported in the prior art, is a brand-new preparation method of the remdesivir intermediate triazinamine derivative, and provides a new synthesis idea for similar compounds of remdesivir.
Klein's Remdesivir-nucleobase synthesis revisited: Chemoselective cyanation of pyrrol-2-carboxaldehyde
Amarante, Giovanni W.,Pereira, Vinicius R. D.,da Silva, Adilson D.,dos Santos, Juliana A.
, p. 1391 - 1395 (2021/06/14)
4-Aminopyrrolo[2,1-f][1,2,4]triazine is a fundamental raw material in the synthesis of remdesivir, which demand has increased due to the tests and potential repositioning of this drug against Coronavirus disease 2019 (COVID-19). Here, three chemical steps route for the preparation of remdesivir's nucleobase is described. Particularly, a highly chemoselective cyanation of Klein's route and successful application of monochloramine prepared from commercial bleach as an N-amination reagent are presented.