Abstract: A conjugate of an anti-HER2 antibody site-specifically modified with a peptide and a chelating agent. The chelating agent is chelated with a metal radionuclide, the peptide and the chelating agent are linked by a linker (L), and the linker (L) does not contain a thiourea bond. A radiopharmaceutical including the conjugate as an active ingredient.

Abstract: Provided is a method for producing a radiohalogen-labeled compound, the method comprises: a step in which a radiohalogen-labeling precursor compound (S-L) having a leaving group (L) capable of being nucleophilically substituted by a radioactive halide ion (X?) is subjected to a radiohalogenation reaction to obtain a reaction mixture RM1 which contains the radiohalogen-labeling precursor compound (S-L) and a reaction product (S—X) resulting from the radiohalogenation reaction; a step in which the reaction mixture RM1 is mixed with a polyvalent acid or a salt thereof to obtain a reaction mixture RM2; and a step in which the reaction product (S—X) is purified from the reaction mixture RM2 by a solid phase extraction method.

Abstract: The present invention provides a process to enhance the productivity such as yield of radioactive fluorine labeled flutemetamol. Provided is a process for producing a radioactive fluorine labeled flutemetamol, which comprises: (a) a step of allowing a labeling precursor represented by the predetermined general formula to react with a radioactive fluoride ion in a presence of a solvent to obtain a radioactive fluorine labeled intermediate represented by the predetermined general formula, and (b) a step of removing the protecting groups from the radioactive fluorine labeled intermediate to obtain a radioactive fluorine labeled flutemetamol, in which the above step (a) is carried out at an internal temperature of reaction solution of 140° C. or higher.

Abstract: Provided is a method for producing a radiohalogen-labeled compound, the method comprises: a step in which a radiohalogen-labeling precursor compound (S-L) having a leaving group (L) capable of being nucleophilically substituted by a radioactive halide ion (X?) is subjected to a radiohalogenation reaction to obtain a reaction mixture RM1 which contains the radiohalogen-labeling precursor compound (S-L) and a reaction product (S—X) resulting from the radiohalogenation reaction; a step in which the reaction mixture RM1 is mixed with a polyvalent acid or a salt thereof to obtain a reaction mixture RM2; and a step in which the reaction product (S—X) is purified from the reaction mixture RM2 by a solid phase extraction method.

Abstract: The present invention provides a process to enhance the productivity such as yield of radioactive fluorine labeled flutemetamol. Provided is a process for producing a radioactive fluorine labeled flutemetamol, which comprises: (a) a step of allowing a labeling precursor represented by the predetermined general formula to react with a radioactive fluoride ion in a presence of a solvent to obtain a radioactive fluorine labeled intermediate represented by the predetermined general formula, and (b) a step of removing the protecting groups from the radioactive fluorine labeled intermediate to obtain a radioactive fluorine labeled flutemetamol, in which the above step (a) is carried out at an internal temperature of reaction solution of 140° C. or higher.

Abstract: Provided is a method for producing flutemetamol including the steps of: reacting a precursor compound represented by a predetermined general formula with a radioactive fluoride to obtain a 18F labeling compound represented by a predetermined general formula; allowing a strong base to act on the reaction mixture of the above step containing the precursor compound and the 18F labeling compound; after the above step, purifying the 18F labeling compound using a reverse phase solid phase extraction cartridge; and removing a protective group to obtain [18F]flutemetamol.

Abstract: Provided is a method for producing flutemetamol including the steps of: reacting a precursor compound represented by a predetermined general formula with a radioactive fluoride to obtain a 18F labeling compound represented by a predetermined general formula; allowing a strong base to act on the reaction mixture of the above step containing the precursor compound and the 18F labeling compound; after the above step, purifying the 18F labeling compound using a reverse phase solid phase extraction cartridge; and removing a protective group to obtain [18F]flutemetamol.