一条通向具有抗疟活性、合成具有挑战性的桥连非手性1,2,4,5-四氧杂环己烷的有效路线。
An efficient route into synthetically challenging bridged achiral 1,2,4,5-tetraoxanes with antimalarial activity.
作者信息
Ellis Gemma L, Amewu Richard, Hall Charlotte, Rimmer Karen, Ward Steven A, O'Neill Paul M
机构信息
Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, UK.
出版信息
Bioorg Med Chem Lett. 2008 Mar 1;18(5):1720-4. doi: 10.1016/j.bmcl.2008.01.053. Epub 2008 Jan 18.
Here we present an efficient route into synthetically challenging bridged 1,2,4,5-tetraoxanes. The key to the success of this route is the use of H(2)O(2) and catalytic I(2) to form the gem-dihydroperoxide followed by a Ag(2)O mediated alkylation using 1,3-diiodopropane. Using this methodology a range of bridged tetraoxanes which display good in vitro antimalarial activity were synthesized.
在此，我们展示了一条合成具有挑战性的桥连1,2,4,5-四氧杂环己烷的有效路线。该路线成功的关键在于使用过氧化氢（H₂O₂）和催化量的碘（I₂）形成偕二氢过氧化物，随后使用氧化银（Ag₂O）介导的1,3-二碘丙烷进行烷基化反应。利用这种方法合成了一系列具有良好体外抗疟活性的桥连四氧杂环己烷。
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