09-06-2023 дата публикации
Номер: CN116239577A
Принадлежит:
The invention provides a method for preparing Cudetaxstat, and belongs to the technical field of medicines. According to the scheme, the method comprises the specific steps that 3-chloro-2-fluoroaniline and chloral hydrate are subjected to condensation, cyclization and reduction reaction to construct an indole parent nucleus, Grignard reaction and ultralow-temperature reaction conditions do not need to be adopted, and meanwhile, 3-((2, 4-difluorophenyl)-1, 2, 3-triazole is optimized. According to the present invention, the reaction conditions in the preparation of 2, 6-dichloro-7-fluoro-1-(1-propyl-1H-pyrazol-4-yl)-1H-indol-3-yl) sulfo)-2-fluoroethyl benzoate and the final product Cudetaxestat are provided; the product purity is 99.85%, and the total yield of the route is 7.05%, which is improved by 10 times compared with the original route. The method provided by the invention has the characteristics of cheap and easily available raw materials, mild reaction conditions, simple post-treatment ...
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