Co-authored scientific publication in “Pharmaceuticals” – TMTHSI in metal-free click chemistry

A study co-authored by TBD and published in “Pharmaceuticals” in August 2023 has detailed the properties and potential applications in metal-free click chemistry for a new compound, tetramethylthiocycloheptyne sulfoximine (TMTHSI). The research was a collaborative effort involving six institutions: Cristal Therapeutics and Maastricht University in The Netherlands, Utrecht University, TBD Pharmatech in Estonia, Lonza AG in Switzerland, and the University of Glasgow in the UK.

The study focused on three main aspects of TMTHSI. First, it examined the compound’s scalability and found that it can be produced in quantities of up to 100 grams. Second, the research looked at the compound’s stability in acidic conditions, specifically its resistance to trifluoroacetic acid (TFA), making it suitable for peptide synthesis. Third, the study explored TMTHSI’s efficiency in the functionalization of antibodies, noting high yield and limited hydrophobicity compared to other alkyne reagents.

The compound was found to be compatible with Good Manufacturing Practices (GMP), an industry standard for pharmaceutical production. The research suggests that TMTHSI has potential for diverse applications in bioconjugation, including the development of new medicines and therapies.

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