Method of preparing ethacrynic amide derivatives and application thereof

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.

Dependencies are inferred from the claim text.