A simple and facile iodination method of didechlorotiacumicin B and aromatic compounds  

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作  者:Haibo Zhang Liping Zhang Imran Khan Guangtao Zhang Yiguang Zhu Changsheng Zhang 

机构地区:[1]Key Laboratory of Tropical Marine Bio-resources and Ecology,Guangdong Key Laboratory of Marine Materia Medica,RNAM Center for Marine Microbiology,South China Sea Institute of Oceanology,Chinese Academy of Sciences,Guangzhou 510301,China [2]Sanya Institute of Oceanology,SCSIO,Yazhou Scientific Bay,Sanya 572000,China [3]Southern Marine Science and Engineering Guangdong Laboratory(Guangzhou),Guangzhou 511458,China [4]University of Chinese Academy of Sciences,Beijing 100049,China

出  处:《Science China Chemistry》2021年第10期1736-1742,共7页中国科学(化学英文版)

基  金:the Key Science and Technology Project of Hainan Province(Key Science and Technology Project ZDKJ202018);the Southern Marine Science and Engineering Guangdong Laboratory(Guangzhou,2019ZD0406);the Chinese Academy of Sciences(QYZDJ-SSW-DQC004);the National Natural Science Foundation of China(81872778,31630004,41911530078);the Ministry of Science and Technology of China(2018YFC1406705)。

摘  要:Tiacumicin B(also known as fidaxomicin or difimicin)is a marketed 18-membered macrolide antibiotic for the treatment of Clostridium difficile infections.Tiacumicin B is structurally characterized with two chlorine atoms substituted on the aromatic ring,which is installed by the halogenase Tia M.During the study on halide compatibility of Tia M,a facile and nonenzymatic iodination method of didechlorotiacumicin B was discovered,requiring Na I,acid and air for iodination at room temperature.This method was also amenable to other 9 aromatic substrates with electron-rich sites for iodination.

关 键 词:IODINATION tiacumicin METAL-FREE facile chemistry 

分 类 号:TQ465[化学工程—制药化工]

 

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