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从简单的基原料中简要合成 (+) -巴塞拉丁B

Brendan T Parr¹, Christos Economou¹, Seth B Herzon¹

¹Department of Chemistry, Yale University, New Haven, Connecticut 06520, USA.

|September 17, 2015

概括

由于的反应性,合成复杂的化物如 (+) - 巴塞拉丁B具有挑战性. 这项研究采用了精简的九步合成,使用芳香异环,避免复杂的保护组.

科学领域:

有机化学
医学化学
自然产品合成

背景情况:

化物是含有的天然产品,具有显著的生物活性.
它们的合成经常受到的反应性阻碍,导致具有保护组的复杂路径.
芳香异环为缓解这些合成挑战提供了潜在的策略.

研究的目的:

开发一种有效的合成抗艾滋病毒化物 (+) - 巴塞拉丁B.
展示使用芳香异环作为合成前体的优点.
通过避免传统的保护群策略来简化化物合成.

主要方法:

使用基于的原料.
使用九步合成序列.
适用于芳异环的杆式关键转换.

主要成果:

在9个步骤中成功合成 (+) - 巴塞拉丁B.
证明了用于复杂类合成的芳香前体的可行性.
突出转换难以和异环.

结论:

芳香异环为简化复杂化合物合成提供了有效的策略.
这种方法简化了生物活性化合物的制备,如 (+) - 巴塞拉丁B.
开发的路线比涉及保护群体的传统方法具有优势.

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