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Title:
IMPROVEMENT OF PREPARATION OF 2-AMINO(2,3,5-TRI-O-BENZYL-BETA-D-ARABINOFURANOSYL)ADENINE
Document Type and Number:
Japanese Patent JPH0665281
Kind Code:
A
Abstract:

PURPOSE: To easily and economically obtain the subject compd. useful as an intermediate of an antileukemic agent by a specified method using a di(trialkylsilylamino)-trialkylsilylpurine as a starting material.

CONSTITUTION: First, a 2,6-di(trialkylsilylamino)-9-trialkylsilylpurine expressed by formula I (with the proviso that alkyl is a 1-4C alkyl) is reacted with 2,3,5-tri- O-benzyl-1-chloro-D-arabinofuranose expressed by formula II preferably at 80 to 85°C for 18 to 30 hours in 1,2-dichloroethane to obtain a 2,6-di(trialkylsilylamino)-9-(2,3,5-tri-O-benzyl-β-D-arabino-furanosyl)purine. Then the obtd. compd. is reacted with a 1-4C alkanol (preferably methanol) in the reaction liquid preferably at 50 to 60°C for 30 to 120 min to obtain the objective compd. expressed by formula III, which is then separated from the liquid.


Inventors:
ANIKA MAAKOBATSUKU
MOORISU PII RAMONTAGUNU
Application Number:
JP14332791A
Publication Date:
March 08, 1994
Filing Date:
June 14, 1991
Export Citation:
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Assignee:
ASH STEVENS INC
International Classes:
A61K31/70; A61K31/7042; C07H19/19; A61K31/7052; A61K31/7076; A61P35/02; C07D473/32; C07F7/10; C07H19/16; C07H23/00; (IPC1-7): C07H19/19
Domestic Patent References:
JPS5429520U1979-02-26
JPS62116582A1987-05-28
Attorney, Agent or Firm:
Akira Asamura (3 outside)