937046-97-4Relevant articles and documents
Process for synthesizing 7 -iodopyrrolo [2,F] [1,m-triazine -4 - amine
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Paragraph 0032-0035, (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.
PYRROLO[2,1-F] [1,2,4] TRIAZIN-4-YLAMINES IGF-1R KINASE INHIBITORS FOR THE TREATMENT OF CANCER AND OTHER HYPERPROLIFERATIVE DISEASES
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Page/Page column 73, (2010/11/27)
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