Pmea and pmpa cyclic producing synthesis

Details Pmea and pmpa cyclic producing synthesis Pmea and pmpa cyclic producing synthesis

C - Chemistry, Metallurgy

07

F

C07F 9/6574 (2006.01) C07F 9/6571 (2006.01)

Patent

CA 2485597

The method of preparing compounds of Formula I is described: Formula Iwherein:M and V are cis to one another and MPO3H2 is a phosphonic acid selected from the group consisting of 9-(2-phosphonylmethoxyethyl)adenine, and (R)-9-(2-phosphonylmethoxypropyl)adenine; wherein V is phenyl, optionally substituted with 1-2 substituents selected from a group consisting of fluoro, chloro, and bromo; comprising:coupling a chiral 1-phenylpropane-1,3-diol, wherein the phenyl may be optionally substituted, with MPOCl2 or an N-6 substituted analogue thereof.Additionally, methods and salt forms are described that enable isolation and purification of the desired isomer.

L'invention concerne un procédé d'élaboration de composés représentés par la formule I, dans laquelle M et V sont mutuellement cis et MPO3H2 est un acide phosphonique appartenant au groupe constitué de 9-(2-phosphonylméthoxyéthyl)adénine et de (R)-9-(2-phosphonylméthoxypropyl)adénine; V est phényle, éventuellement substitué par 1 ou 2 substituants appartenant au groupe constitué de fluoro, chloro, et bromo. Le procédé consiste à coupler un 1-phénylpropane-1,3-diol chiral, sachant que phényle peut être éventuellement substitué, par MPOCl¿2? ou un analogue correspondant substitué en N-6. L'invention concerne également des procédés et des formes de sels qui permettent d'isoler et de purifier l'isomère recherché.

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