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Bioorthogonal conjugation chemistry and derivatization of reagents for labeling molecules. (a) [4+2] cycloaddition reaction between trans-cyclooctene (TCO) and 1,2,4,5-tetrazine (Tz) moieties to give the 1,4-dihydropyridazine adduct. (b) Derivatization of TCO-OH to the corresponding TCO-NHS carbonate. (c) Derivatization of Tz-BnNH2 to the corresponding Tz-NHS ester. (d) Labeling of amine-containing molecules with Tz or TCO (R = MNP, peptide, small-molecule, etc.).
