文档介绍：
Tetracyclic Xanthone Derivatives via One-Pot Cascade
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YU Fuchao, ZHANG Qianqian, ZHANG Yichuan, YAN Shengjiao*, LIN Jun***
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(Key Laboratory of Medicinal Chemistry for Natural Resources (Yunnan University), Ministry
of Education, School of Chemical Science and Technology, Yunnan University,
KunMing 650091)
Abstract: A procedure for the synthesis of highly functional tetracyclic xanthone derivatives is
described. A concise and efficient one-pot synthesis of structurally diverse tetracyclic xanthones was
constructed by treating different types of heterocyclic ketene aminals with 3-formylchromone using
catalytic Et3N in acetone at room temperature. The advantages of this method include high efficiency,
mild reaction conditions and environmentally benign reagents. These xanthones are promising
candidates for drug discovery. Consequently, a library of diverse tetracyclic xanthones was rapidly
constructed using the present protocol and this concise process presented herein has great potential to
be applied to parallel synthesis in drug discovery.
Keywords: tetracyclic xanthone; one-pot; cascade reaction; heterocyclic ketene aminals;
3-formylchromone
INTRODUCTION
The xanthone substructure is of great significance, as natural products[1] such as cratoxylum
cochinchinense have been used in traditional medicines to treat fever, itching,