Synthesis of acyclic nucleoside derivatives

Details Synthesis of acyclic nucleoside derivatives Synthesis of acyclic nucleoside derivatives

C - Chemistry, Metallurgy

07

D

C07D 473/18 (2006.01)

Patent

CA 2339250

Novel intermediates and improvements in the synthesis of acyclic guanine nucleoside prodrugs of the formula (R)-9-[(2-alkanoylmethyl)-4-(aminoacyloxy)butyl]guanine (for example valtamociclovir stearate), including purine salts amenable to one pot alkylation with the acyclic side chain, acyclic 2-amino-6-halo-purine and protected guanine precursors, one pot manipulations thereof and last step work up procedures.

La présente invention concerne de nouveaux intermédiaires et des améliorations apportées à la synthèse de promédicaments à nucléoside de guanine acyclique de formule (R)-9-[(2-alkanoylméthyl)-4-(aminoacyloxy)butyl]guanine (par exemple, valtamociclovir stréarate), y compris des sels puriques susceptibles d'être soumis à une alkylation en pot avec la chaîne latérale acyclique, la 2-amino-6-halo-purine acyclique et des précurseurs de guanine protégée, à une manipulation en pot et aux dernières étapes de l'élaboration.

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