Patent ID: 8067648
Filing Date: 2011-11-29
Classification: C07B,C07C,Y10T

Abstract:
1. A method for synthesizing a radioactive ligand having a 18 F-labeled fluorobenzene ring of general formula (7), comprising the steps of: (A) reacting a phenylhalide compound of general formula (1) wherein X is Br or I; R 1 , R 2 , R 3 , R 4 and R 5 may be the same or different and each represent a hydrogen atom, an alkyl group or a heteroatom-containing functional group, provided that all of R 1 , R 2 , R 3 , R 4 and R 5 are not a hydrogen atom or an alkyl group, with a trialkyltin of general formula (2) wherein R 10 represents an alkyl group in the presence of a palladium catalyst to obtain a phenyltin compound of general formula wherein X, R 1 , R 2 , R 3 , R 4 , R 5 and R 10 are as defined above; (B) oxidizing an iodobenzene compound of general formula (4) wherein E represents a functional group which donates electron to a π electron system, and n is 1, 2, 3, 4 or 5, and then reacting the oxidized compound with toluenesulfonic acid monohydrate to obtain a hydroxytosyliodobenzene compound of general formula (5) wherein Ts represents a toluenesulfonyl group; and E and n are as defined above; (C) reacting the hydroxytosyliodobenzene compound of general formula (5) with the phenyltin compound of general formula (3) to obtain a diphenyliodonium salt of general formula (6) wherein R 1 , R 2 , R 3 , R 4 , R 5 , E, n and Ts are as defined above; and (D) reacting the diphenyliodonium salt of general formula (6) with [ wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined above.