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Title:
SYNTHESIS OF 9-(2-HYDROXYETHOXYMETHYL)GUANINE
Document Type and Number:
Japanese Patent JP3753447
Kind Code:
B2
Abstract:

PURPOSE: To obtain guanine compounds for anti-virus agent or the like in high efficiency by protecting guanine derivatives with trimethylsilyl group in an aprotic solvent under the presence of a catalyst, deblocking after reacting with acyloxyethoxy-methylhalogenide and hydrolyzing.
CONSTITUTION: Guanine or their salts are reacted with 2 to 4 times mole of hexamethyldisilazane in the presence of the aprotic solvent and a catalyst amount of ammonium sulfate to protect an amino group with trimethylsilyl group, then reacted with the stoichiometric amount of the acyloxyethoxymethylhalogenide at 50-100°C without isolating the trimethylsilyl derivateves. The trimethylsilyl protecting group is removed by hydrolysis using aqueous solution of sodium acetate or sodium hydroxide, the subject 9-(2- hydroxyethoxymethyl)guanine expressed by the formula is obtained in good yield by hydrolyzing the 9-(2-acetoxyethoxymethyl)guanine free from purification, in NaOH aqueous solution.


Inventors:
ティベリオ ブルツエセ
ジウセッペ グアツイ
マルコ ロニヨニ
ジウリアーノ マルコン
Application Number:
JP1994000308681
Publication Date:
March 08, 2006
Filing Date:
December 13, 1994
Export Citation:
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Assignee:
SOLAR CHEMICAL S.A.
International Classes:
C07D473/18; C07B61/00; (IPC1-7): C07D473/18; //C07B61/00
Domestic Patent References:
JP51054589A
Foreign References:
Attorney, Agent or Firm:
金田 暢之
伊藤 克博
石橋 政幸