A series of 4‐sulfoximinocyclopent‐2‐en‐1‐ones were prepared in 35 to 99% yield through a calcium(II)‐catalyzed aza‐Piancatelli reaction, including in enantioenriched form. Depending on their substitution pattern, diverse diastereoselective chemical transformations can be applied to these scaffolds, allowing access to cyclopentane derivatives. This study opens synthetic routes to cyclopentane‐based scaffolds and also paves the way for the exploration of the associated chemical space in drug discovery.

中文翻译：

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钙 （II） 催化合成亚砜酰胺环戊烯酮


通过钙 （II） 催化的 aza-Piancatelli 反应，以 35% 至 99% 的产率制备一系列 4-磺胺酰氨基环戊-2-烯-1-酮，包括对映体富集形式。根据它们的取代模式，可以将不同的非对映选择性化学转化应用于这些支架，从而获得环戊烷衍生物。这项研究为基于环戊烷的支架开辟了合成途径，也为探索药物发现中的相关化学空间铺平了道路。