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Method Of Preparing Ethacrynic Amide Derivatives And Application Thereof
Patent

Method Of Preparing Ethacrynic Amide Derivatives And Application Thereof

National Tsing Hua University, 俞鐘山, Chen, Jenn-Tzong, Chiang, Li-Wu, Huang, Hao-Lien, Lin, Wuu-Jyh, Wang, Wei-Ting, Chen, Gon-Shen, Yeh, Chun-Nan, Huang, Yin-Cheng, …
19/06/2013

Abstract

The present invention provides a method for preparing [18F]—N-(4-fluorobutyl)ethacrynic amide which is prepared from radiofluorination and deprotection of the precursor tosylate N-Boc-N-[4-(toluenesulfonyloxy)-butyl)ethacrynic amide], obtained from ethacrynic acid via 6-step synthesis in 39% yield, in a radiochemical yield of 44%, aspecific activity of 48 GBq/μmol and radiochemical purity of 98%. The present invention further provides a composition for positron emission tomography (PET) of an animal models of a tumor liver or a liver disease, comprising [18F]—N-(4-fluorobutyl)ethacrynic amide and a pharmaceutically acceptable carrier.

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