发明授权
US5892063A Cephalomannine epoxide, its analogues and a method for preparing the same
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Cephalomannine环氧化物,其类似物及其制备方法
- 专利标题: Cephalomannine epoxide, its analogues and a method for preparing the same
- 专利标题(中): Cephalomannine环氧化物,其类似物及其制备方法
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申请号: US861286申请日: 1997-05-21
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公开(公告)号: US5892063A公开(公告)日: 1999-04-06
- 发明人: Qun Y. Zheng , Christopher K. Murray , Randall J. Daughenbaugh
- 申请人: Qun Y. Zheng , Christopher K. Murray , Randall J. Daughenbaugh
- 申请人地址: CO Boulder
- 专利权人: Hauser, Inc.
- 当前专利权人: Hauser, Inc.
- 当前专利权人地址: CO Boulder
- 主分类号: A61K31/335
- IPC分类号: A61K31/335 ; A61K31/337 ; A61P35/00 ; C07D305/14 ; C07D407/12
摘要:
An antitumor compound of formula (5) ##STR1## in which R is Ac or H, and R.sub.1, R.sub.2 is an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu, R.sub.3 is H; R.sub.1 and R.sub.2 and R.sub.3 are H; R.sub.1 is an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu, R.sub.2, R.sub.3 is H; R.sub.1 and R.sub.3 are H, R.sub.2 is an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu; R.sub.1 is H, R.sub.2 and R.sub.3 are an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu; R.sub.1 and R.sub.2 and R.sub.3 are an alkyl group Me, Et, Pr, i-Pr, n-Bu or t-Bu. Me is an abbreviation for methyl, Et is ethyl, Pr is propyl, i-Pr is isopropyl, n-Bu is n-butyl, and t-Bu is tert-butyl. Also provided by the invention is a one step method of preparing a compound of formula (5) whereby a taxane having a tiglate group attached to the side chain is contacted with an oxidizing reagent resulting in the formation of an epoxide having antitumor activity.
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