| 摘要 |
NEW MATERIAL:A compound of formula I (R<1> is ethyl or isopropyl; R<2> and R<3> are each H, 1-3C alkyl or Cl; X is O or S; Z is S or methylene; when X is O and Z is S, R<2> and R<3> are not H at the same time). EXAMPLE:5-Ethyl-1-[(2-hydroxyethoxy)methyl]-6-phenylthio-2-thiouracil. USE:An activiral agent. In particular, having marked effects on retrovirus, and low toxic to host cells. PREPARATION:A reaction is made at -80 to 10 deg.C in a solvent such as THF between a compound of formula II (R<4> is protective group for hydroxyl) and an organoalkali metal (e.g. lithium diisopropylamide). Thence, an arylthio- modifier (e.g. diphenyldisulfide) is reacted under conditions similar to those for said organoalkali metal to eliminate the protective groups, thus obtaining the objective compound of the formula I (where Z is S). |
