Preparation method for (2'R)-2'-deoxy-2'-fluoro-2'-methyluridine

A technology of methyl ureaside and dibenzoyl ureaside, which is applied in the preparation of sugar derivatives, chemical instruments and methods, sugar derivatives, etc., can solve problems such as the utilization rate of chemical atoms with short route and cost, and achieve low product cost. , The chemical synthesis route is short, and the purity is good.
CN104710491AInactive Publication Date: 2015-06-17NINGBO CHEMGOO PHAMA TECH +1
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
NINGBO CHEMGOO PHAMA TECH
Publication Date
2015-06-17
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention belongs to the technical field of organic chemistry, and relates to a preparation method for (2'R)-2'-deoxy-2'-fluoro-2'-methyluridine. The preparation method for (2'R)-2'-deoxy-2'-fluoro-2'-methyluridine comprises the steps: with a protective fluororibose (represented by the formula I) as a starting material, carrying out a condensation reaction with a raw material ditrimethylsiyl protective uracil (represented by the formula VI) to obtain dibenzoyl uridine (represented by the formula IV), de-protecting dibenzoyl uridine to obtain the target product uridine (represented by the formula V), wherein a reaction equation is described in the specification. Compared with the prior art, the method reduces one reaction step in synthesis steps firstly, improves the production efficiency in the large-scale production, reduces the workload, reduces energy consumption and three-waste emission load, and improves the total yield of preparing the compound represented by the formula V from the compound represented by the formula I.
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Description

Technical field

[0001] The invention belongs to the technical field of organic chemistry, and relates to a preparation method of (2'R)-2'-deoxy-2'-fluoro-2'-methyluridine. Background technique

[0002] (2'R)-2'-deoxy-2'-fluoro-2'-methyluridine (Formula V) is the key intermediate of Sofosbuvir, a drug for the treatment of chronic hepatitis C virus (HCV) infection. The traditional literature preparation method is mainly to protect the fluororibose (formula I) as the starting material, after reductive acylation, and then with the TMS derivative of N-benzoylcytosine (formula II) to produce Protect cytidine (formula III), protect cytidine (formula III) and then undergo high-temperature hydrolysis to obtain dibenzoyl uridine (formula IV), and then deprotect the dibenzoyl uridine (formula IV) to obtain the target product urea Glycoside (Formula V) (Document 1: J. Med. Chem. 2010, 53, 7202-7218; Document 2: J. Med. Chem. 2005, 48, 5504-5508). The reaction formula is as follows

[0003] ...

Claims

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