Institute of Organic Chemistry Polish Academy of Sciences, Kasprzaka 44/52, Warsaw 01-224, Poland.
Chem Commun (Camb). 2020 May 28;56(43):5718-5734. doi: 10.1039/d0cc01771j. Epub 2020 May 11.
Strain-release driven transformations give access to attractive bioisosteric motifs highly prized by medicinal chemists and they are characteristic of molecules possessing distorted bond lengths and angles. By broadening the chemical space in drug discovery, recently, these compounds have attracted a lot of interest. Their reactivity stems mainly from an increased energy and destabilization. As a result, the opening of the bridging bond occurs under the action of both nucleophiles and electrophiles as well as radical species and transition metals. Though the bridge bond dominates their reactivity, it is also influenced by the substitution pattern. This feature article focuses on strain-release driven strategies paying particular attention to the most recent (year > 2010) advances.
应变释放驱动的转化可获得医学化学家高度重视的有吸引力的生物等排基序，它们是具有扭曲键长和键角的分子的特征。通过拓宽药物发现中的化学空间，这些化合物最近引起了广泛关注。它们的反应性主要源于能量增加和不稳定性增加。因此，在亲核试剂和亲电试剂以及自由基和过渡金属的作用下，桥键打开。虽然桥键主导它们的反应性，但它也受到取代模式的影响。本文重点介绍应变释放驱动的策略，特别关注最近（> 2010 年）的进展。
