The present invention relates to a method for providing a
single isomer chemical entity targeting vector suitable for providing a
label of the targeting vector. The method applies a specific combination between dienes and dienophiles with complementary reverse
electron demand Diels-
Alder cycloaddition reactivity that will form a
single isomer form of the compound after
ligation and then oxidation. The labeled
single isomer chemical entity targeting vectors are useful in therapy, radiotherapy, therapeutic diagnosis, diagnosis, and imaging. The methods employ
click chemistry in which one chemical entity conjugated to the
label is clicked together with a second chemical entity having complementary anti-
electron demand Diels-
Alder cycloaddition reactivity that is conjugated to a targeting carrier and then rapidly oxidized to form a single isomeride compound.