Hypervalent radioactive astatine or iodine compounds, and preparation methods thereof

摘要

The present invention relates to a compound having formula (I): wherein: —X is in particular 125I Or 211At; —R1 and R′1 are independently from each other chosen preferably from the group consisting of electron-withdrawing groups and alkyl groups; —R2 is chosen from the group consisting of: H, alkyl groups, functional groups being able to bind a vector, and functional groups having targeting properties which make the compound of the invention a vector itself; —Z is a heteroatom, R5, R8 and R9 are preferably H; —Y is preferably an electron withdrawing group.;

主权项

1. A compound having formula (I): wherein: X is a radioisotope selected from the group consisting of: 125I, 123I, 124I, 131I, and 211At; R1 and R′1 are independently from each other selected from the group consisting of nitro, acyl, formyl, sulfonyl, cyano, chloride, bromide, fluoride, OAc, an alkyl group, OH, NH2, or R1 and R′1 form together with the adjacent carbon atom carrying them a C═O group; R2 is selected from the group consisting of: H, an alkyl group, a functional group that binds a vector selected from the group consisting of maleimide, N-hydrosuccinimide ester, tetrafluorophenyl ester, isothiocyanate, isocyanate, anhydride, alkyne, an azide group, and a functional group having targeting properties selected from the group consisting of biotin, hapten, an antibody, an antibody fragment, a peptide, a drug, and a nanocarrier; R8 and R9 are independently selected from the group consisting of H, OH, NH2, halogen, an alkyl group, an alkoxy group, an amine group, an amide group, and an ester group; Z is a heteroatom selected from the group consisting of O and NH; and R5 is H or a C(R6)(R7) radical forming together with Y and X a five-membered heterocycle wherein:
when R5=H, Y is an electron withdrawing group selected from the group consisting of nitro, acyl, formyl, sulfonyl, trifluoromethyl, cyano, chloride, bromide, fluoride, and OAc; orwhen R5=C(R6)(R7) radical forming together with Y and X a five-membered heterocycle, Y is selected from O and NH and R6 and R7 are as defined above for R1 and R′1.