2'-fluoro nucleotide

Abstract

The present invention provides a 2'-fluor-nucleoside compound used for curing hepatitis b infection, hepatitis c infection, HIV and abnormal cells proliferation including tumour and cancer. The compound has formulas (I), (II), (III), (IV) or its medicine salt, wherein, base is purine or pyrimidine base; R<1> is OH, H, OR<3>, N<3>, CN, halogen includes F, or CF3, lower alkyl, amino, lower alkyl amino, two lower alkyl amino, or alkoxy; R<2> is H, phosphate, including monophosphate, diphosphate, triphosphate or stable phosphate prodrug; acyl, or other medical leaving group, when human body uses, the group provides a compound which R<2> is H or phosphate; sulfonic ester includes alkyl or aralkyl sulfonyl, including methyl sulphonyl, benzyl, wherein, benzyl is selectively substituted by the substituent of one or more aryl definition, lipid, amino, peptide or cholesterin; and R<3> is acyl, alkyl, phosphate or other medical leaving group, it is a group cracked by the parent compound when the human body uses.

Description

[0001] This application is a divisional application of the international application date of February 25, 1999, the international application number of PCT / US99 / 04051 (the national application number is 99805472.0), and the invention name of "2'-fluoronucleoside". [0002] The invention described herein was made with government support under Grant No. AI32351 awarded by the State Department of Health. The United States Government has affirmed the rights to this invention. technical field [0003] The invention belongs to the field of medicinal chemistry, and specifically includes 2'-fluoronucleoside and its preparation method and use. Background technique [0004] For some years, synthetic nucleosides such as 5-iodo-2'-deoxyuridine and 5-fluoro-2'-deoxyuridine have been used to treat cancer and herpes viruses. Since the 1980s, synthetic nucleosides have also been beneficial in the treatment of HIV, hepatitis and Epstein-Barr virus. [0005] In 1981, Acquired Immune Deficie...

AI Technical Summary

Problems solved by technology

At least with respect to 2′-ribofuranosyl nucleosides, this may be due to the previous perception that placing the fluorine group in the 2′-ribofuranosyl configuration was difficult

For L-2'-fluoro-2',3'-unsaturated purine nucleosides, it may be due to the instability of purine nucleosides in acidic media, resulting in the cleavage of the glucosyl bond

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