Many cyclobutane natural products have intriguing biological properties that arise from their fascinating chemical structures. Cyclobutane natural products feature a cyclobutane scaffold as the core or as a part of the spirocyclic or fused cyclic core. However, the highly functionalized nature and the inherent stereochemistry of these cyclobutane natural products, which are associated with their biological activities, pose tremendous challenges to their preparation. In this perspective, we present contemporary advancements in synthetic methods and/or strategies en route to the bioactive cyclobutane natural products. We begin by describing the representative bioactive cyclobutane natural products and then focus on illustrative examples of their syntheses reported from 2018 to 2021. These advances will enable efficient syntheses of cyclobutanes of structural and biological importance.

许多环丁烷天然产物具有有趣的生物学特性，这些特性源于其迷人的化学结构。环丁烷天然产物以环丁烷骨架为核心或作为螺环或稠环核心的一部分。然而，这些与其生物活性相关的环丁烷天然产物的高度功能化性质和固有的立体化学对其制备提出了巨大挑战。从这个角度来看，我们在途中展示了合成方法和/或策略的当代进步具有生物活性的环丁烷天然产物。我们首先描述具有代表性的生物活性环丁烷天然产物，然后重点介绍 2018 年至 2021 年报告的其合成的示例。这些进展将使具有结构和生物学重要性的环丁烷的有效合成成为可能。