Nucleotide analog composition and synthesis method

Details Nucleotide analog composition and synthesis method Nucleotide analog composition and synthesis method

C - Chemistry, Metallurgy

07

F

C07F 9/6561 (2006.01) A61K 31/675 (2006.01) A61P 31/12 (2006.01) C07D 473/34 (2006.01)

Patent

CA 2298059

The invention provides a composition comprising bis(POC)PMPA and fumaric acid (1:1). The composition is useful as an intermediate for the preparation of antiviral compounds, or is useful for administration to patients for antiviral therapy or prophylaxis. The composition is particularly useful when administered orally. The invention also provides methods to make PMPA and intermediates in PMPA synthesis. Embodiments include lithium t-butoxide, 9-(2-hydroxypropyl) adenine and diethyl p-toluenesulfonylmethoxy-phosphonate in an organic solvent such as DMF. The reaction results in diethyl PMPA preparations containing an improved by-product profile compared to diethyl PMPA made by prior methods.

L'invention concerne une composition comprenant de la 9-[2-(R)- [[Bis[[(isopropoxycarbonyl)oxy]méthoxy]phosphinoyl]méthoxy]propyl]adénine ("bis(POC)PMPA") et de l'acide fumarique (1: 1). Cette composition est utile comme intermédiaire dans l'élaboration de composés antiviraux, ou bien pour l'administration à des patients en guise de thérapie ou de prophylaxie antivirale. Elle est particulièrement utile en administration orale. L'invention concerne également des procédés relatifs à l'élaboration de la (R)- 9-[2-(phosphonométhoxy) propyl]adénine ("PMPA") et des intermédiaires pour la synthèse de la PMPA. Parmi les variantes figurent le t-butoxyde de lithium, la 9-(2-hydroxypropyl) adénine et le diéthyl p-toluènesulfonylméthoxy-phosphonate dans un solvant organique comme le diméthylformamide. La réaction donne des préparations de diéthyl PMPA ayant un profil de sous-produit amélioré par rapport aux procédés utilisés antérieurement pour l'élaboration de diéthyl PMPA.

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