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Title:
PROCESS FOR PREPARING 1(3-AZIDO2,3-DIDEOXY-BETAD-ERYTHROPENTAFURANOSIL) THIMINE AND ITS RELATED COMPOUND
Document Type and Number:
Japanese Patent JPH03209393
Kind Code:
A
Abstract:

PURPOSE: To obtain the subject compound having an antiviral activity and especially useful for AIDS by reacting a specific compound with an organic halogenocompound, treating the reaction product with a diester of an azodicarboxylic acid and phosphine, etc., opening ring and deblocking.

CONSTITUTION: A compd. of formula I (R1 is H, alkyl, alkoxy, hydroxyalkyl or halogen) is reacted with a derivative of the formula of R2X [R2 is trithyl, (1-3C mono- or dialkoxy), trithyl, pixyl, (R3R4R5)Si (R3-R5 are each 1-5C alkyl)] to obtain a compd. of formula II. This compd. is converted by the action of a diester of an azodicarboxylic acid and phosphine or a phosphite derivative in a solvent to obtain a compd. of formula III. The ring of this compound is opened in a solvent in the presence of a metal azide to obtain a compd. of formula IV and the subject compd. of formula V is obtained by deblocking the 5' functional group thereof.


Inventors:
SUTANISURASU CHIERUNETSUKI
JIYANNMARUKU BARERI
Application Number:
JP29166990A
Publication Date:
September 12, 1991
Filing Date:
October 29, 1990
Export Citation:
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Assignee:
UNIV PARIS CURIE
International Classes:
C07H9/06; A61K31/70; A61K31/7042; A61K31/7052; A61K31/7064; A61K31/7072; A61P31/12; A61P31/18; C07H19/06; (IPC1-7): A61K31/70; C07H9/06; C07H19/06
Attorney, Agent or Firm:
Kazuo Sato (2 outside)