2'-METHYLIDENEPYRIMIDINE NUCLEOSIDE COMPOUND AND DRUG USE THEREOF

摘要

NEW MATERIAL:A compound shown by formula I (R<1> is amino or OH; when R<1> is amino, R<2> is halogen, 2-4C alkynyl or lower alkyl and when R<1> is OH, R<2> is 2-4C alkyl, 2-4C alkynyl or haloalkyl; R3 is H or phosphoric acid residue). EXAMPLE:2'-Deoxy-2'-methylidene-5-fluorocytiaine. USE:A carcinostatic agent. PREPARATION:Hydroxyl groups at saccharide part 3' position and 5' position of a compound shown by formula II (R is halogen, alkyl, haloalkyl or 2-4C alkynyl) is protected and then hydroxyl group at saccharide 2' position is oxidized. Then the resulting substance is reacted with Wittig reagent to give a saccharide 2' position methylidene derivative, then protecting groups at saccharide 3' position and 5' position are removed and optionally hydroxyl group at saccharide 5' position is phoshorylated.