Tetrahydroisoquinoline natural products are a kind of alkaloids containing various pharmacological activities. These structurally diverse alkaloids mainly consist of two subclasses, monotetrahydroisoquinolines (MTHI) and bistetrahydroisoquinolines (BTHI). Since its family member, Ecteinascidin-743 (INN: Trabectedin, trade name: Yondelis®), has been approved by European Union in 2007 and the FDA in 2015 for the treatment of advanced soft tissue tumors, the research on this kind of natural product is full of new vitality. Quinocarcin and lemonomycin share a common diazabicyclo[3.2.1]octane framework that belongs to the subclass of MTHI, and their excellent antitumor activity and challenging architecture have made them an ideal target for total synthesis. In this short review, the progress in the total synthesis of quinocarcin and lemonomycin is summarized.

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四氢异喹啉生物碱喹诺卡星和柠檬霉素的全合成研究进展

四氢异喹啉天然产物是一类具有多种药理活性的生物碱。这些结构多样的生物碱主要由两个亚类组成：单四氢异喹啉（MTHI）和双四氢异喹啉（BTHI）。自其家族成员Ecteinascidin-743（INN：Trabectedin，商品名：Yondelis®）于2007年获得欧盟批准、2015年获得FDA批准用于治疗晚期软组织肿瘤以来，对该类天然产物的研究不断深入充满了新的活力。喹诺卡星和柠檬霉素具有共同的二氮杂双环[3.2.1]辛烷骨架，属于MTHI亚类，其优异的抗肿瘤活性和具有挑战性的结构使它们成为全合成的理想靶标。这篇简短的综述总结了喹诺卡星和柠檬霉素的全合成进展。