Process

Details Process Process

C - Chemistry, Metallurgy

07

D

260/242.3

C07D 473/00 (2006.01) C07F 9/547 (2006.01)

Patent

CA 2026238

B2847/Abs Abstract A process for the preparation of a compound of formula (A): Image (A) wherein X is hydrogen, hydroxy, chloro, C1-6 alkoxy or phenyl C1-6 alkoxy and Ra and Rb are hydrogen, including acyl and phosphate derivatives thereof; which process comprises: i) the preparation of a compound of formula (I): Image ( I ) wherein R1 is C1-6 alkyl, or phenyl C1-6 alkyl in which the phenyl group is optionally substituted; R2 is hydrogen, hydroxy, chlorine, C1-6 alkoxy, phenyl C1-6 alkoxy or amino; and R3 is halogen, C1-6 alkylthio, - 2 - 32847/Abs C1-6 alkylsulphonyl, azido, an amino group or a protected amino group, which process comprises the reaction of a compound of formula (II): Image (II) with a compound of formula (VII): Image (VII) wherein Q is a leaving group, J is hydrogen or halo and R1 is as hereinbefore defined; to give a compound of formula (VIII): Image (VIII) followed by reduction of the compound of formula (VIII) to give a compound of formula (I) as hereinbefore defined; and, as necessary or desired, interconverting variables R1, R2 and R3 to further values of R1, R2 and R3; - 3 - B2847/Abs (ii) the conversion of the resulting compound of formula (I) to a compound of formula (A) by converting variable R3, when other than amino, to amino, reducing the ester groups CO2R1 to CH2OH and optionally forming acyl or phosphate derivatives thereof, and as necessary or desired converting variable R2 in the compound of formula (I) to variable X in the compound of formula (A).

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