发明名称 |
Process for the preparation of ribonucleotide reductase inhibitors |
摘要 |
The present invention is directed toward a novel process of preparing 2'-exocyclic vinylfluoride derivatives of cytidine analogues for use as ribonucleotide reductase inhibitors. The novel process of the present invention utilizes a cytidine derivative as the required starting material and provides the ribonucleotide reductase inhibitor in a more efficient than the reaction sequence. The process is more efficient than the process disclosed by McCarthy et al. in European Patent Application Publication No. 0 372 268 published Jun. 13, 1990, in that it requires fewer chromatographies and results in an overall yield of greater than 25% for the five steps. The present invention further provides the ribonucleotide reductase inhibitor in a four step reaction sequence and results in an overall yield of greater than 35%.
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申请公布号 |
US5589587(A) |
申请公布日期 |
1996.12.31 |
申请号 |
US19950419315 |
申请日期 |
1995.04.10 |
申请人 |
MERRELL PHARMACEUTICALS INC. |
发明人 |
MCCARTHY, JAMES R.;MATTHEWS, DONALD P.;SABOL, JEFFREY S.;MCCONNELL, JAMES R.;DONALDSON, RICHARD E.;DUQUID, ROBERT |
分类号 |
C07D405/04;C07H1/00;C07H19/06;C07H23/00;(IPC1-7):C07H1/00 |
主分类号 |
C07D405/04 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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