Improved process for preparing 9-substituted derivatives of...

C - Chemistry – Metallurgy – 07 – D

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260/242.3

C07D 473/02 (2006.01) C07D 473/00 (2006.01)

Patent

CA 1096863

Callada Hungary ABSTRACT A process for preparing the 9-(2-hydroxyethoxymethyl) derivatives of guanine and 2-amino-adenine comprising hydrolysing in the presence of a base a compound of formula (II) Image (II) wherein R1 is hydroxy or Image , and X1 and X2 are the same or different and each represent an alkyl or phenyl group, and R2 is hydrogen or Image , provided that when R1 is hydroxy, R2 is hydrogen. The compounds of formula (II) are novel intermediates and are prepared by reacting guanine, or 2-amino adenine in which the 2 and 9, or 2,6 and 9 positions respectively are acylated, with a diester of 2-oxa-1,4-butanediol in the presence of a catalytic amount of a strong acid.

285592

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