Abstract
Reaction of cyclopropanated trans-cyclooctene (cpTCO) with in situ generated ortho-quinone is an efficient tool for bioorthogonal protein conjugation. The (4+2)-cycloaddition of cpTCO with ortho-quinone is significantly faster than its cyclooctyne counterpart (BCN). Orthogonal, tandem cpTCO-quinone and BCN-azide cycloadditions afforded a homogeneous, dual labelled antibody-drug conjugate.
Original language | English |
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Pages (from-to) | 7338-7341 |
Journal | Chemical Communications |
Volume | 54 |
Issue number | 53 |
DOIs | |
Publication status | Published - 1 Jan 2018 |