We present a novel and effective photocatalytic method for the methylation of β-diketones with controllable degrees of deuterium incorporation via development of new methyl sources. By utilizing a methylamine-water system as the methyl precursor a...
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A Concise Synthetic Approach to Highly Reactive Click‐to‐Release Trans‐ Cyclooctene Linkers
Von Wiley-VCH zur Verfügung gestellt
An increase of the click-to-release reaction rate between cleavable trans-cyclooctenes (TCO and tetrazines would be beneficial for drug delivery applications. In this work, we developed a short and stereoselective synthesis route towards highly reactive sTCOs that serve as cleavable linkers, affording quantitative tetrazine-triggered payload release. In addition, the 5-fold more reactive sTCO exhibited the same in vivo stability as the parent TCO linker when used as antibody linker in circulation in mice.
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