- Synthesis of a functionalized oxabicyclo[2.2.1]-heptene-based chemical library
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The 7-oxabicyclo[2.2.1]heptene ring system is a common structural motif in many pharmacologically interesting molecules. We recognized the potential to employ this highly oxygenated and conformationally-restricted scaffold in diversity-oriented synthesis to generate a library of non-chiral but topologically complex compounds. Herein, we report the synthesis and biological evaluation of two 96-member tricyclic libraries containing the oxabicyclo[2.2.1]heptene framework using acetal formation as the key step.
- Luesse, Sarah B.,Wells, Gregg,Miller, Jeanne,Bolstad, Erin,Bergmeier, Stephen C.,McMills, Mark C.,Priestley, Nigel D.,Wright, Dennis L.
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- 5. 6 - double-dehydrogenation to a spot maomao mellow derivative and its anti-tumor application
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The invention provides a 5, 6-bidehydronorcantharides alcohol derivative and application thereof to tumor resistance. The 5, 6-bidehydronorcantharides alcohol derivative has the structural formula as shown in the formula I as described in the description, wherein R is selected from -H or -CH2COOH. Activity tests prove that the 5, 6-bidehydronorcantharides alcohol derivative I designed and synthesized by the invention has a favorable anti-hepatoma effect and is expected to be applied as an antitumor cantharidin drug in clinic. In addition, the novel synthesis method for the compound has the advantages of available raw materials, low cost, simple synthesis route, high yield and convenience in operation and implementation.
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Paragraph 0037-0039
(2017/08/24)
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