发明名称 |
Antimalarial analogs of artemisinin |
摘要 |
A process for synthesizing oxygen-containing polyoxatetracycle compounds and in particular analogs of the antimalarial agent known as qinghaosu or artemisinin is disclosed. The process employs as a reactant an olefinically unsaturated bicyclic bridging ketone having nonenolizable bridgehead moieties for both of its alpha positions. This ketone is converted to a vinylsilane that is subjected to ozonolytic cleavage of its olefinic bond to yield a member of a family of unique carboxyl/carbonyl-substituted vinylsilanes which may in turn optionally be subjected to a wide range of reactions prior to a final ozonolysis/acidification step which closes the oxygen-containing ring structure. The various intermediates are claimed as aspects of this invention as are novel tetracycles and their use as antimalarials.
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申请公布号 |
US5019590(A) |
申请公布日期 |
1991.05.28 |
申请号 |
US19890414730 |
申请日期 |
1989.09.27 |
申请人 |
SRI INTERNATIONAL |
发明人 |
AVERY, MITCHELL A.;CHONG, WESLEY K. M. |
分类号 |
C07D491/18;C07D493/04;C07D493/18;C07D495/18 |
主分类号 |
C07D491/18 |
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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