Synthesis of acyclic nucleosides

Details Synthesis of acyclic nucleosides Synthesis of acyclic nucleosides

C - Chemistry, Metallurgy

07

D

C07D 473/18 (2006.01) C07D 473/00 (2006.01) C07D 473/32 (2006.01) C07F 7/10 (2006.01)

Patent

CA 2243826

A method for preparing enhanced bioavailability antiviral compounds of formula (I) where one of R1 and R2 is -C(O)CH(CH(CH3)2)NH2 or -C(O)CH(CH(CH3)CH2CH3)NH2 and the other of R1 and R2 is -C(O)C3-C21 saturated or monounsaturated, optionally substituted alkyl; and R3 is OH or H, the method comprising: A) the monodeacylation of a diacylated compound corresponding to formula (I) wherein R1 and R2 are both -C(O)CH(CH(CH3)2)NH2 or -C(O)CH(CH(CH3)CH2CH3)NH2 (which are optionally N-protected) or R1 and R2 are both -C(=O)C3-C21, saturated or monounsaturated, optionally substituted alkyl; B) acylating the thus liberated side chain 4-hydroxy or side chain 2-hydroxymethyl group with the corresponding - C(O)CH(CH(CH3)2)NH2 or -C(O)CH(CH(CH3)CH2CH3)NH2 or -C(=O)C3-C21, saturated or monounsaturated, optionally substituted alkyl to thereby produce a compound of formula (I); and C) deprotecting as necessary.

Méthode de préparation de composés antiviraux à biodisponibilité renforcée de la formule (I). Dans cette formule, R1 ou R2 correspond à -C(O)CH(CH(CH3)2)NH2 ou -C(O)CH(CH(CH3CH2CH3)NH2 tandis que l'autre élément correspond à un alkyle facultativement substitué, saturé ou monoinsaturé -C(O)C3-C21 et R3 correspond à OH ou H. La méthode comprend les étapes suivantes: a) monodéacylation d'un composé diacylé correspondant à la formule (I), considérant que R1 et R2 correspondent l'un et l'autre à -C(O)CH(CH(CH3)2NH2 ou -C(O)CH(CH(CH3)CH2CH3)NH2 (facultativement protégés en N) ou bien correspondent l'un et l'autre à un alkyle facultativement substitué, saturé ou monoinsaturé -C(=O)C3-C21; b) acylation du groupe 4-hydroxy de chaîne latérale ou 2-hydroxyméthyle de chaîne latérale ainsi libéré avec l'alkyle facultativement substitué, saturé ou monoinsaturé -C(O)CH(CH(CH3)2)NH2 ou -C(O)CH(CH(CH3)CH2CH3)NH2 correspondant, pour obtenir un composé de la formule (I); c) supprimer la protection selon les nécessités.

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