Department of Chemistry "Ugo Schiff", University of Florence, Via della Lastruccia 13, 50019 Sesto Fiorentino, Florence, Italy.
Org Biomol Chem. 2019 Jan 31;17(5):1037-1052. doi: 10.1039/c8ob02808g.
Natural products (NPs) have been shown to be an extraordinary source of bioactive compounds and three-dimensional complex frameworks that can be useful to produce high-value molecular collections that are able to address "undruggable" and difficult therapeutic targets. Bicyclic acetals are particularly relevant for these purposes, given their key role in several biological interactions and the structural and stereochemical diversity that comes from the many possible ring combinations. To investigate this topological diversity, we have systematically characterized in a systematic and detailed manner fused, spiro and bridged bicyclic acetals in a large set of NPs, highlighting the great potential of bicyclic acetals in Diversity-Oriented Synthesis (DOS). Accordingly, a summary of some recent efforts on the development of acetal-containing small molecule collections through DOS approaches is herein reported.
天然产物（NPs）已被证明是生物活性化合物和三维复杂结构的非凡来源，可用于生成高价值的分子集合，以解决“不可成药”和治疗困难的靶点。双环缩醛在这方面特别相关，因为它们在几种生物相互作用中起着关键作用，并且结构和立体化学的多样性来自于许多可能的环组合。为了研究这种拓扑多样性，我们系统地、详细地描述了大量 NPs 中融合、螺环和桥接双环缩醛，突出了双环缩醛在定向合成（DOS）中的巨大潜力。相应地，本文总结了一些通过 DOS 方法开发含缩醛小分子集合的最新研究进展。
