Amido analogs of geldanamycin, an ansamycin anticancer agent, were designed, synthesized, and assayed with SKBR3 cells, in which stability of HER2 receptor tyrosine kinase is dependent on the chaperone Hsp90. An amide was employed as a trisubstituted alkene isostere at the C8,9 position, which provi
Synthesis of (+)-8a,9-secoartemisinin and related analogs
✍ Scribed by Mitchell A. Avery; Wesley K.M. Chong; George Detre
- Publisher
- Elsevier Science
- Year
- 1990
- Tongue
- French
- Weight
- 198 KB
- Volume
- 31
- Category
- Article
- ISSN
- 0040-4039
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✦ Synopsis
An efficient synthesis of (+)-8a,9-secoartemisinin 2. a ring-D cleaved, tricyclic analog of (+)-artemisinin 1. has been accomplished. Dioxetane 7, produced upon ozonolysis of vinyl-silane 5 in methanol, was intercepted with acid to provide the stable bicyclic peroxy-aldehyde ~, which was readily converted to the title compound(s).
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## Abstract A general scheme for the synthesis of 4,4′‐diaminodiphenylsulfone‐d~5~ (Dapsone) from aniline‐d~5~ is described. The method may have general application and the preparation of the related analogs, 4,4′‐dimethylaminodiphenyl sulfone from aniline‐d~5~ and 4,4′‐dimethoxydiphenyl sulfone fr