METHOD AND KIT FOR PREPARING TECHNETIUM-99M COMPLEXES

摘要

PCT No. PCT/US91/02450 Sec. 371 Date Aug. 21, 1992 Sec. 102(e) Date Aug. 21, 1992 PCT Filed Apr. 10, 1991.The invention relates to a method of preparing a radiolabelled technetium complex by bringing Tc-99m in the form of a pertechnetate solution in a complex-forming reaction with a compound of the general formula (I) wherein R1-R12 each independently represents a hydrogen atom, a C1-C4 alkyl group, a carboxy group, or a carboxy(C1-C4)alkyl group; or wherein R1+R2, R3+R4, R5+R6, R7+R8, R9+R10 and R11+R12 each independently represent an oxo or imino function; and wherein furthermore: R13 is a hydrogen atom, a C1-C4 alkyl group or a carboxy(C1-C4)alkyl group; R14 is a hydrogen atom or an amino group; n is 0, 1 or 2; A represents an amino group or a mercapto group; and B represents a mercapto group, or a group of the general formula NH-Z-CO-NH-mZ-COOH, wherein: Z is an optionally substituted C1-C4 alkylene, cycloalkylene or alkylidene group, and m is an integer from 0 to 20; with the provisos: (i) that at least one substituent selected from the group consisting of R1-R13 and B is or comprise a carboxy group; and (ii) that R3+R4 or R7+R8 represents an oxo function or both R3+R4 and R7+R8 or both R5+R6 and R7+R8 represent oxo functions, if A is an amino group and B is a group of the formula NH-Z-CO-NH-mZ-COOH; by performing said reaction in the presence of Sn(II) as a reducing agent, in the absence of a transfer agent, in an at least substantially aqueous solvent system having a pH of at least 10, and at ambient temperature. The invention further relates to a kit for performing said method.