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没有使用保护组的海洋自然产品的总合成

Phil S Baran¹, Thomas J Maimone, Jeremy M Richter

¹Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Road, La Jolla, California 92037, USA. pbaran@scripps.edu

|March 23, 2007

概括

化学家现在可以有效地合成复杂的天然产品,使用一种新的无保护组策略. 这种方法显著减少了合成步骤,为生物研究提供了大量的对抗分子纯化合物.

科学领域:

有机化学有机化学
合成化学合成化学
自然产品的合成自然产品的合成

背景情况:

有机合成的进步还没有完全解决生产复杂分子用于研究的挑战.
复杂的自然产品的高效合成对于生物和医学研究至关重要.

研究的目的:

为复杂的自然产品开发一种无保护组的,对复杂的自然产品进行抗选择的总合成策略.
在步数和产量方面证明这种新方法的效率.

主要方法:

开发了一种无保护组的合成路径.
执行了Hapalindole,Fischerindole,Welwitindolinone和模糊家族的对抗选择性总合成.
专注于准备性规模的合成.

主要成果:

在十个步骤或更短的时间内实现目标天然产品家族的总合成.
产生大量单个反体,与以前的方法相比,这是一个显著的改进.
消除了保护群体的需要,降低了成本和复杂性.

结论:

开发的无保护组策略使复杂分子的高效合成成为可能.
这种方法显著缩短了合成路径,并增加了对体纯化合物的产量.
展示的原理可以应用于合成其他复杂的分子架构.

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