发明名称 NOVEL NUCLEOSIDE CONTAINING CYCLOPENTENE RING
摘要 PURPOSE:A compound shown by the formula I (R is OH, or H; B is nucleic acid base of thymine, 4-thiouracil or 5-iodouracil when R is OH, and B is nucleic acid base of thymine, uracil, cytosine, guanine, or 4-thiouracil when R is H) and its salt. EXAMPLE:1-[(1R,2S,3R)-2,3-Dihydroxy-4-hydroxymethyl-4-cyclopen-t-en-1- yl]-5-me thyl-2,4(1H,3H)pyrimidinedione. USE:A carcinostatic agent. PREPARATION:A compound shown by the formula II is reacted with a 3-lower alkoxy-2-methylacryloyl isocyanate in a solvent such as DMF, etc. under cooling -30--50 deg.C to give a compound shown by the formula III (R2-R4 are OH- protecting group; R5 is lower alkyl), which is subjected to ring closured, the protecting group is eliminated, to give a compound shown by the formula I where B is thymine and R is OH.
申请公布号 JPS6187674(A) 申请公布日期 1986.05.06
申请号 JP19840210151 申请日期 1984.10.06
申请人 YOSHITOMI PHARMACEUT IND LTD;TOYO JOZO CO LTD 发明人 ONO MASAJI;ARITA MASAFUMI;SAKAKIBARA HIDEO;FUKUKAWA SEISHI
分类号 C07D473/18;A61K31/505;A61P35/00;C07D239/47;C07D239/54;C07D239/56 主分类号 C07D473/18
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