Sharjah Institute for Medical Research, University of Sharjah, P.O. Box 27272, Sharjah, UAE.
College of Arts and Sciences, Department of Biology, Chemistry and Environmental Sciences, American University of Sharjah, Sharjah, UAE.
Chemistry. 2019 Dec 10;25(69):15710-15735. doi: 10.1002/chem.201902596. Epub 2019 Sep 20.
Diversity-oriented synthesis (DOS) has become a powerful synthetic tool that facilitates the construction of nature-inspired and privileged chemical space, particularly for sp -rich non-flat scaffolds, which are needed for phenotypic screening campaigns. These diverse compound collections led to the discovery of novel chemotypes that can modulate the protein function in underrepresented biological space. In this context, starting material-driven DOS is one of the most important tools used to build diverse compound libraries with rich stereochemical and scaffold diversity. To this end, ene/yne tethered salicylaldehyde derivatives have emerged as a pluripotent chemical platform, the products of which led to the construction of a privileged chemical space with significant biological activities. In this review, various domino transformations employing o-alkene/alkyne tethered aryl aldehyde/ketone platforms are described and discussed, with emphasis on the period from 2011 to date.
导向多样性合成（DOS）已成为一种强大的合成工具，可促进受自然启发的和有利的化学空间的构建，特别是对于需要进行表型筛选的富含 sp 的非平面支架。这些多样化的化合物集合导致了新型化学型的发现，这些化学型可以调节在代表性不足的生物空间中的蛋白质功能。在这种情况下，基于起始材料的 DOS 是用于构建具有丰富立体化学和支架多样性的多样化化合物库的最重要工具之一。为此，烯/炔键合水杨醛衍生物已成为一种多功能化学平台，其产物导致构建了具有重要生物活性的有利化学空间。在这篇综述中，描述并讨论了各种采用邻烯烃/炔键合芳基醛/酮平台的多米诺转化，重点是 2011 年至今的时期。
