Methods for the synthesis of substituted purines

Details Methods for the synthesis of substituted purines Methods for the synthesis of substituted purines

C - Chemistry, Metallurgy

07

D

C07D 473/34 (2006.01) C07D 473/16 (2006.01) C07D 473/18 (2006.01) C07D 473/36 (2006.01) C07D 473/40 (2006.01)

Patent

CA 2463507

The invention provides general methods for preparing 2,9-, 2,6,9-, O6-aryl- and O6-alkyl-substituted purines in a combinatorial and traceless fashion. The methods involve, in some embodiments, Mitsunobu alkylation of 2-fluoro-6- phenylsulfenylpurine at N9 with alcohols in solution, followed by C2-capture of the purine core with a resin-bound amine and subsequent oxidation and displacement of the C6 sulfonyl group with amines and anilines.

Cette invention concerne des méthodes générales de préparation de purines substituées par 2,9-, 2,6,9-, O?6¿-aryle- et O?6¿-alkyle- selon un mode combinatoire et sans trace. Ces méthodes font intervenir, dans certains modes de réalisation, une alkylation Mitsunobu de 2-fluoro-6-phénylsulfenylpurine à N9 avec des alcools en solution, suivie d'une capture C2 du noyau purique avec une amine liée à une résine, après quoi on procède à l'oxydation et au déplacement du groupe sulfonyle C6 avec des amines et des anilines.

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