2,5-二取代双环[2.1.1]己烷作为刚性环戊烷变体
2,5-disubstituted bicyclo[2.1.1]hexanes as rigidified cyclopentane variants.
作者信息
Paul Shashwati, Adelfinsky Daniel, Salome Christophe, Fessard Thomas, Brown M Kevin
机构信息
Department of Chemistry, Indiana University 800 E. Kirkwood Ave Bloomington IN 47405 USA
SpiroChem AG Rosental Area, WRO-1047-3, Mattenstrasse 22 4058 Basel Switzerland.
出版信息
Chem Sci. 2023 Jul 12;14(30):8070-8075. doi: 10.1039/d3sc02695g. eCollection 2023 Aug 2.
Identification of rigid counterparts for common flexible scaffolds is crucial to the advancement of medicinal chemistry. Here we showcase a new class of building blocks, 2,5-disubstituted bicyclo[2.1.1]hexanes that can act as rigidified -, or -1,3-disubstituted cyclopentanes, common motifs in drugs. The scalable synthesis of these structures was enabled through the use of C-H functionalization logic and cycloaddition reactions.
确定常见柔性支架的刚性类似物对于药物化学的发展至关重要。在此，我们展示了一类新型的结构单元，即2,5-二取代双环[2.1.1]己烷，它可以作为药物中常见的刚性化的1,3-二取代环戊烷类似物。通过使用C-H官能化策略和环加成反应实现了这些结构的可扩展合成。
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