Preparation method of baloxavir marboxil intermediate compound

A technology of compounds and intermediates, applied in the direction of organic chemistry, can solve the problems of polluting synthesis methods, dangers, etc., and achieve the effects of optimizing purification steps, reducing production costs and unit prices, good commercial value and industrial development potential
CN110305091AActive Publication Date: 2019-10-08JIANGSU UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
JIANGSU UNIV OF TECH
Publication Date
2019-10-08

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Abstract

The invention relates to a preparation method of a baloxavir marboxil intermediate compound. The preparation method includes: using 2-methyl-3-benzyloxy-4-oxo-4-hydropyrane as the initial raw materialand oxygen as the oxidizing agent to perform oxidizing reaction under the effect of a nitric oxide catalyst to generate 3-benzyloxy-4-oxo-4-hydropyrane-2-formaldehyde, and performing further oxidization to obtain the product 3-benzyloxy-4-oxo-4-hydropyrane-2-methyl carboxylate. The preparation method has the advantages that product purification steps are optimized, the raw materials of the methodis cheap and easy to obtain, and the method is simple in post-processing steps, capable of avoiding extra production cost, capable of greatly lowering production cost and product unit price, capableof favorably promoting the researches and development of various medicine intermediates using the product as the raw material and good in commercial value and industrial development potential.
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Description

technical field

[0001] The invention relates to the technical field of organic synthesis of pharmaceutical intermediates, in particular to a method for preparing a baloxavir intermediate compound, namely methyl 3-benzyloxy-4-oxo-4-hydropyran-2-carboxylate . Background technique

[0002] Baloxavir is a new anti-influenza drug approved by the US FDA in 2018 [WO 2017221869; AU2017282305; JP 6212678; CN 109311911;], its English name is Xofluza, or baloxavirmarboxil, is a new type of small molecule drug that can Effectively treat patients (aged ≥ 12 years) with uncomplicated acute influenza within 48 hours. The treatment effect is very obvious. According to experts, the new drug only needs 1 tablet, which is equivalent to the effect of 10 tablets of the current conventional treatment drug. Baloxavir (Young-A Heo. Baloxavir: First Global Approval [J]. Drugs, 2018, 78, 693-697.).

[0003] Therefore, the demand for baloxavir will also increase, and the currently reported syntheti...

Claims

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