2. Academic Validation
  3. TMTHSI, a superior 7-membered ring alkyne containing reagent for strain-promoted azide-alkyne cycloaddition reactions

TMTHSI, a superior 7-membered ring alkyne containing reagent for strain-promoted azide-alkyne cycloaddition reactions

  • Chem Sci. 2020 Aug 10;11(33):9011-9016. doi: 10.1039/d0sc03477k.
Jimmy Weterings 1,  Cristianne J F Rijcken 1,  Harald Veldhuis 2,  Tommi Meulemans 2,  Darya Hadavi 3,  Matt Timmers 1,  Maarten Honing 3,  Hans Ippel 4,  Rob M J Liskamp 1 4 5 6
Affiliations

Affiliations

  • 1 Cristal Therapeutics Oxfordlaan 55 6229 EV Maastricht The Netherlands robert.liskamp@cristaltherapeutics.com.
  • 2 Mercachem Kerkenbosch 1013 6546 BB Nijmegen The Netherlands.
  • 3 The Maastricht Multimodal Molecular Imaging Institute (M4I), Maastricht University Universiteitssingel 50 6229 ER Maastricht The Netherlands.
  • 4 Department of Biochemistry, CARIM, Maastricht University Universiteitssingel 50 6229 ER Maastricht The Netherlands.
  • 5 School of Chemistry, Joseph Black Building, University of Glasgow University Avenue Glasgow G12 8QQ UK robert.liskamp@glasgow.ac.uk.
  • 6 Chemical Biology and Drug Discovery, Department of Pharmaceutics, Utrecht University Universiteitsweg 99 3584 CG Utrecht The Netherlands.
PMID: 34123155 DOI: 10.1039/d0sc03477k
Abstract

We describe the development of TMTH-SulfoxImine (TMTHSI) as a superior click reagent. This reagent combines a great reactivity, with small size and low hydrophobicity and compares outstandingly with existing click reagents. TMTHSI can be conveniently functionalized with a variety of linkers allowing attachment of a diversity of small molecules and (peptide, nucleic acid) biologics.

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