C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 19/173 (2006.01) C07D 473/40 (2006.01)
Patent
CA 2400470
2-Chloro-9-(2-deoxy-2-fluoro-.beta.-D-arabinofuranosyl)-9H-purin-9-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro- D-arabinofuranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy-2-fluoro-.beta.-D-arabinofuranosyl)- 9H-purin-6-amine. When the purine reactant is substituted in the 6 position with a halogen, a reaction step with an alkoxide is carried out prior to the reaction with ammonia.
L'invention concerne la synthèse de la 2-Chloro-9-(2-déoxy-2-fluoro- beta -D-arabinofuranosyl)-<i>9H</i>-purine-9-amine consistant à faire réagir une purine 2-chloro-6-substituée avec un 2-déoxy-2-fluoro-D-arabinofuranose protégé et activé; et à faire réagir avec une base telle que l'ammoniac en vue d'obtenir la 2-chloro-9-(2-déoxy-2-fluoro- beta -D-arabinofuranosyl)-<i>9H</i>-purine-6-amine. Lorsque le réactant de purine est substitué en position 6 par un halogène, l'étape de la réaction s'effectue avec un alcoxyde préalablement à la réaction avec l'ammoniac.
Fowler Anita T.
Montgomery John A.
Secrist John A. III
Moffat & Co.
Southern Research Institute
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