Process for preparing 9-(2-hydroxyethoxymethyl)-guanine, and int

Details Process for preparing 9-(2-hydroxyethoxymethyl)-guanine, and int Process for preparing 9-(2-hydroxyethoxymethyl)-guanine, and int

1985-12-11

1987-10-20

Rizzo, Nicholas S.

Organic compounds -- part of the class 532-570 series

Organic compounds

Four or more ring nitrogens in the bicyclo ring system

544276, 544277, C07D47318

Patent

active

047015268

ABSTRACT:
There is disclosed a process for preparing 9-(2-hydroxyethoxymethyl)-guanine (acyclovir) of the formula IV ##STR1## wherein a novel compound of the formula I ##STR2## wherein R and R' may be the same or different and represent hydrogen, (C.sub.1 -C.sub.8)acyl or benzyl and R.sub.1 represents (C.sub.1 -C.sub.8)acyl, is hydrolyzed under mild basic conditions. Also disclosed is the novel compound of the formula I, a process for the preparation thereof by condensing a novel compound of the formula II ##STR3## with a compound A--CH.sub.2 --O--CH.sub.2 CH.sub.2 --OR' (A is a leaving group, Q is hydrogen or a leaving group), the novel compound of the formula II and a process for the preparation thereof by means of condensing glyoxal hydrate and a compound of the formula V ##STR4##

REFERENCES:
patent: 4495190 (1985-01-01), Hagberg et al.

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