Biologically active compounds and pharmaceutically relevant intermediates often feature sterically congested stereogenic centers, in particular, carbon stereocenters that are either tertiary tetrasubstituted ones or quaternary in nature. Synthons that comprise such bulky and often structurally complex core units are of high synthetic value and represent important incentives for communities connected to drug discovery and development. Streamlined approaches that give access to a diverse set of compounds incorporating acyclic bulky stereocenters are relatively limited, though vital. They enable further exploration of three-dimensional entities that can be designed and implemented in discovery programs, thereby extending the pool of molecular properties that is inaccessible for flat molecules. However, the lack of modular substrates in particular areas of chemical space inspired us to consider functionalized heterocycles known as cyclic carbonates and carbamates as a productive way to create sterically crowded alkenes and stereocenters.

中文翻译：

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乙烯基和炔基取代的杂环作为过渡金属促进的立体选择性合成中的优先支架

生物活性化合物和药学相关中间体通常具有空间拥挤的立体中心，特别是本质上是叔四取代或季的碳立体中心。包含如此庞大且结构通常复杂的核心单元的合成子具有很高的合成价值，并且代表了与药物发现和开发相关的社区的重要激励措施。尽管至关重要，但能够获得包含无环庞大立构中心的多种化合物的简化方法相对有限。它们能够进一步探索可以在发现程序中设计和实现的三维实体，从而扩展平面分子无法获得的分子特性库。然而，化学空间特定领域缺乏模块化底物促使我们考虑将称为环状碳酸酯和氨基甲酸酯的官能化杂环作为创建空间拥挤的烯烃和立构中心的有效方法。