Method for synthesizing 5-trifluoro methyl-2'-desugarized uridine

A technology of deoxyuridine and trifluoromethyl, applied in sugar derivatives, organic chemistry, etc., can solve the problems of easy pollution of the environment, and achieve the effect of simple operation, easy availability of synthetic raw materials, and high purity
CN100334100CInactive Publication Date: 2007-08-29FUBANG BIO PHARMA HANGZHOU

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
FUBANG BIO PHARMA HANGZHOU
Publication Date
2007-08-29
Estimated Expiration
Not applicable · inactive patent

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Abstract

The present invention relates to the synthesis process of 5-trifluoromethyl-2'-dexoy uridine. The compound is prepared with 2'-dexoy uridine as initial material and through iodizing, hydroxyl protection, trifluoromethylation and deprotection. The said process of the present invention has easy-to-obtain material, simple synthesis and no pollution.
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Description

Technical field:

[0001] The invention relates to the field of drug synthesis, in particular to a synthesis method of 5-trifluoromethyl-2'-deoxyuridine. Background technique:

[0002] 5-Trifluoromethyl-2'-deoxyuridine (Trifluridine), also known as trifluridine or trifluorothymidine, is clinically used as an antiviral drug and is a thymidine analog that interferes with DNA synthesis, It is effective for primary keratoconjunctivitis and recurrent keratitis caused by herpes simplex virus types I and II. At the same time, it is an important intermediate for the preparation of the compound 5-trifluoromethyl-2', 3'-dideoxyuridine (5-trifluoromethyl-2'3'-dideoxyuridine) with high specificity against hepatitis B virus body. 5-trifluoromethyl-2', 3'-dideoxyuridine was developed by Bayer, and in Chinese patent application 92102448.7, a synthetic 5-trifluoromethyl-2', 3'-dideoxyuridine was disclosed The method of glucoside, it is starting raw material with ethyl trifluoropropionate, ...

Claims

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