Baloxvir intermediate and preparation method thereof

By optimizing the synthetic route of baloxavir ester, compound 7 was reacted with R-OH to generate compound 8, which was then reacted with a dehydrating agent to generate compound 9. Finally, the R group was removed to generate baloxavir. This solved the problems of high impurities and high production costs of chiral isomers, and achieved high-yield and low-cost industrial production.

CN122036752APending Publication Date: 2026-05-15CHENGDU BRILLIANT PHARMA CO LTD +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
CHENGDU BRILLIANT PHARMA CO LTD
Filing Date
2024-11-14
Publication Date
2026-05-15

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Abstract

The invention provides a novel intermediate for synthesizing baloxvir and baloxvir dipivoxil and a preparation method of the novel intermediate. According to the method, a compound 7 is used as a starting material, and a new intermediate compound 8 is prepared in the presence of a lithium salt. According to the preparation method of the compound 8 provided by the invention, the use of a Grignard reagent is avoided, industrial amplification is safer, and treatment is easier. Meanwhile, the invention provides an intermediate compound 8-5, the intermediate compound 9-5 prepared from the intermediate compound 8-5 has a higher dr value and yield, the content of isomer impurities of baloxvir is reduced, the difficulty of later purification of baloxvir is greatly reduced, the yield of later purification of baloxvir is greatly increased, and the production cost is reduced.
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