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    Process for the preparation of purine derivatives as antiviral agents
    134.
    发明授权
    Process for the preparation of purine derivatives as antiviral agents 失效
    用于制备作为抗病毒剂的嘌呤衍生物的方法

    公开(公告)号：US5220024A

    公开(公告)日：1993-06-15

    申请号：US588569

    申请日：1990-09-26

    申请人： Graham R. Geen ,  Trevor J. Grinter ,  Stephen Moore

    发明人： Graham R. Geen ,  Trevor J. Grinter ,  Stephen Moore

    IPC分类号： C07D473/18 ,  C07D473/00 ,  C07D473/22 ,  C07D473/24 ,  C07D473/32 ,  C07D473/36 ,  C07D473/40 ,  C07F9/6561

    CPC分类号： C07D473/00

    摘要： A process for the preparation of a compound of formula (A): ##STR1## wherein X is hydrogen, hydroxy, chloro, C.sub.1-6 alkoxy or phenyl C.sub.1-6 alkoxy and R.sub.a and R.sub.b are hydrogen, including acyl and phosphate derivatives thereof; which process comprises:i) the preparation of a compound of formula (I): ##STR2## wherein R.sub.1 is C.sub.1-6 alkyl, or phenyl C.sub.1-6 alkyl in which the phenyl group is optionally substituted; R.sub.2 is hydrogen, hydroxy, chlorine, C.sub.1-6 alkoxy, phenyl C.sub.1-6 alkoxy or amino; and R.sub.3 is halogen, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphonyl, azido, an amino group or a protected amino group, which process comprises the reaction of a compound of formula (II): ##STR3## with a compound of formula (VII): ##STR4## wherein Q is a leaving group, J is hydrogen or halo and R.sub.1 is as hereinbefore defined; to give a compound of formula (VIII): ##STR5## 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 R.sub.1, R.sub.2 and R.sub.3 to further values of R.sub.1, R.sub.2 and R.sub.3 ;(ii) the conversion of the resulting compound of formula (I) to a compound of formula (A) by converting variable R.sub.3, when other than amino, to amino, reducing the ester groups CO.sub.2 R.sub.1 to CH.sub.2 OH and optionally forming acyl or phosphate derivatives thereof, and as necessary or desired converting variable R.sub.2 in the compound of formula (I) to variable X in the compound of formula (A).