Synthesis of polysubstituted bicyclo[2.1.1]hexanes enabling access to new chemical space,Chemical Science |
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Synthesis of polysubstituted bicyclo[2.1.1]hexanes enabling access to new chemical space,Chemical Science
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Saturated bridged-bicyclic compounds are currently under intense investigation as building blocks for pharmaceutical drug design. However, the most common methods for their preparation only provide access to bridgehead-substituted structures. The synthesis of bridge-functionalised species is highly challenging but would open up many new opportunities for molecular design. We describe a photocatalytic cycloaddition reaction that provides unified access to bicyclo[2.1.1]hexanes with 11 distinct substitution patterns. Bridge-substituted structures that represent ortho-, meta-, and polysubstituted benzene bioisosteres, as well as those that enable the investigation of chemical space inaccessible to aromatic motifs can all be prepared using this operationally simple protocol. Proof-of-concept examples of the application of the method to the synthesis of saturated analogues of biorelevant trisubstituted benzenes are also presented.
中文翻译：
目前正在对饱和桥联双环化合物作为药物设计的构建模块进行深入研究。然而，最常见的制备方法仅提供桥头取代结构的途径。桥功能化物质的合成极具挑战性，但将为分子设计开辟许多新的机会。我们描述了一种光催化环加成反应，该反应提供了对具有 11 种不同取代模式的双环[2.1.1]己烷的统一访问。代表邻位、间位和多取代苯生物电子等排体的桥取代结构，以及那些能够研究芳香族基序无法接近的化学空间的结构，都可以使用这种操作简单的方案来制备。还介绍了应用该方法合成生物相关三取代苯的饱和类似物的概念验证示例。 |
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