Frontier Institute of Science and Technology, Xi'an Jiaotong University, Xi'an 710049, P. R. China.
Department of Medicinal Chemistry, School of Pharmacy, Xi'an Jiaotong University, Xi'an, 710061, China.
Nat Prod Rep. 2021 Sep 23;38(9):1589-1617. doi: 10.1039/d0np00086h.
Total synthesis of natural products has greatly contributed to natural product research, organic synthesis and drug discovery and development. However, in most cases, the efficiency of total synthesis is far from sufficient for direct practical industrial application. Thus, designing a concise and efficient synthetic route with balanced efforts between building the complex skeleton and introducing functional groups is highly desirable. In this critical review, we first present an introduction of this issue and a philosophical framework that cover possible synthetic approaches. Next, we have chosen the biogenetically closely related, biologically important and synthetically extremely challenging natural products, tiglianes, daphnanes and ingenanes as the particular case for the discussion, since in the past 40 years many synthetic approaches have been reported. The successes and pitfalls included therefore serve as the basis to draw some conclusions that may inspire future development in this area.
天然产物的全合成极大地促进了天然产物研究、有机合成和药物发现与开发。然而，在大多数情况下，全合成的效率远远不足以直接应用于实际工业生产。因此，设计一条简洁高效的合成路线，在构建复杂骨架和引入功能团之间取得平衡，是非常理想的。在这篇评论中，我们首先提出了一个问题介绍和一个涵盖可能的合成方法的哲学框架。接下来，我们选择了生物亲缘关系密切、生物意义重大且合成极具挑战性的天然产物，即千里光烷、瑞香烷和穿心莲烷作为讨论的特例，因为在过去的 40 年里，已经有许多合成方法被报道。因此，包括成功和失败在内的这些案例为我们提供了一些结论的基础，这些结论可能会为这一领域的未来发展提供启示。
