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Novel synthesis of beta-nucleosides

A technology of nucleoside compounds and compounds, applied in the direction of drug combinations, organic active ingredients, peptide/protein ingredients, etc., can solve problems such as unsatisfactory

Active Publication Date: 2010-11-10
PHARMAESSENTIA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

none of which are satisfactory

Method used

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  • Novel synthesis of beta-nucleosides
  • Novel synthesis of beta-nucleosides
  • Novel synthesis of beta-nucleosides

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Embodiment Construction

[0051] The present invention relates to an efficient method for the stereoselective synthesis of 2'-deoxynucleosides, more specifically, gemcitabine, and novel intermediates produced in this method.

[0052] Conventional chemical transformations can be used to practice the invention. Those skilled in the art can determine the appropriate chemicals, solvents, protecting groups and reaction conditions for these chemical transformations. Related information is described, for example, in R. Larock, Comprehensive Organic Transformations, VCH Publishers (1989); T.W. Greene and P.G.M. Wuts, Protective Groups in Organic Synthesis, 3rd ed., John Wiley and Sons (1999); L. Fieser and M. Fieser, Fieser and Fieser's Reagents for Organic Synthesis, John Wiley and Sons (1994); and Encyclopedia of Reagents for Organic Synthesis, edited by L. Paquette, John Wiley and Sons (1995) and later editions. For purposes of illustration, specific embodiments of the methods of the invention are describe...

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Abstract

This invention relates to a process of stereoselectively synthesizing -nucleoside, e.g., 2'-deoxy-2,2'-difluorocytidine.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Provisional Application 60 / 985,754, filed November 6, 2007, and US Provisional Application 61 / 023,566, filed January 25, 2008. The contents of the two provisional applications are fully incorporated herein for reference. Background technique [0003] 2'-Deoxynucleosides and their analogs are therapeutically important agents. For example, gemcitabine, ie, 2'-deoxy-2,2'-difluorocytidine, is useful in the treatment of viral infections and cancer. See, eg, US Patents 4,526,988 and 4,808,614. [0004] In general, each 2'-deoxynucleoside has more than one chiral center and can occur as multiple stereoisomers. Not all stereoisomers are therapeutically active. Several stereoselective synthetic routes to 2-deoxy-β-nucleosides have been developed. None of them are satisfactory. [0005] There is a need to develop more efficient routes for the stereoselective synthesis of 2'-deoxynucleo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7076A61K38/20A61K38/21
CPCC07H15/18C07H19/06A61P31/12A61P35/00
Inventor C-Y·朱W-D·李W·李C·K·黄
Owner PHARMAESSENTIA CORP