Artemisinin and its semi-synthetic derivatives have been the corner-stone of malaria chemotherapy. Their life-saving therapeutic effects and characteristic structure bearing a peroxide bridge in a sesquiterpene lactone framework have attracted the attention of both synthetic chemists and synthetic biologists. In this highlighted review, the engineered biosynthesis, chemoenzymatic synthesis, total synthesis and derivatization via site-selective C–H functionalization are outlined as state-of-the-art approaches for the artificial production of artemisinin and its derivatives. To gain rapid and flexible access to the chemical space relevant to artemisinins, two synthetic campaigns that produce both skeletally diverse tetracyclic peroxides and 6-aza-artemisinins are summarized.

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青蒿素的合成和结构多样化，以产生有效的抗疟疾药物

青蒿素及其半合成衍生物一直是疟疾化疗的基石。它们的挽救生命的治疗作用和在倍半萜内酯骨架中带有过氧化物桥的特征结构吸引了合成化学家和合成生物学家的关注。在这篇重点综述中，工程化的生物合成，化学酶法合成，全合成和通过位点选择性C–H功能化的衍生化概述了人工生产青蒿素及其衍生物的最新方法。为了快速，灵活地进入与青蒿素有关的化学领域，总结了两种合成方法，它们同时产生骨骼上不同的四环过氧化物和6-氮杂-青蒿素。