Southern University of Science and Technology, School of Medicine, Shenzhen, 518055, People's Republic of China.
Division of Life Science, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong 999077, China.
Org Biomol Chem. 2021 May 5;19(17):3791-3812. doi: 10.1039/d1ob00448d.
Many natural products have intriguing biological properties that arise from their fascinating chemical structures. However, the intrinsic complexity of the structural skeleton and the reactive functional groups on natural products pose tremendous challenges to chemical syntheses. Semi-synthesis uses chemical compounds isolated from natural sources as the starting materials to produce other novel compounds with distinct chemical and medicinal properties. In particular, advancements in various types of sp3 C-H bond functionalization reactions and skeletal rearrangement methods have contributed to the re-emergence of semi-synthesis as an efficient approach for the synthesis of structurally complex bioactive natural products. Here, we begin with a brief discussion of several bioactive natural products that were obtained via a semi-synthetic approach between 2008 and 2015 and we then discuss in-depth contemporary advancements in the semi-synthesis of bioactive terpenoids and steroids reported during 2016-2020.
许多天然产物具有有趣的生物特性，这些特性源于其迷人的化学结构。然而，天然产物结构骨架的内在复杂性和反应性功能基团对化学合成构成了巨大的挑战。半合成使用从天然来源中分离出的化合物作为起始原料，生成具有独特化学和药用性质的其他新型化合物。特别是，各种类型的 sp3 C-H 键功能化反应和骨架重排方法的进步，使得半合成重新成为合成结构复杂的生物活性天然产物的有效方法。在这里，我们首先简要讨论了 2008 年至 2015 年间通过半合成方法获得的几种生物活性天然产物，然后深入讨论了 2016 年至 2020 年间报道的生物活性萜类和甾体的半合成的当代进展。
