MercachemSyncom summer publications

This summer, the efforts of our scientists led to several new publications and patents. Check them out!

Resulting from the fruitful collaboration between Cristal Therapeutics, Maastricht University and Mercachem, a fast copper-free click reagent has been prepared. In the key step, both the alkyne- and sulfoximinehandle are formed in a one-pot procedure.
TMTHSI, a superior 7-membered ring alkyne containing reagent for strain-promoted azide-alkyne cycloaddition reactions
Chem. Sci. 2020

For the University of Oslo we have evolved a lead Tankyrase inhibitor, in next iterations of design-make-test cycles to optimize ADME- and minimize off-target properties, into a pre-clinical candidate.
Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor
J. Med. Chem.
2020, 63, 6834-6846

To study the effects of the effects of thyroid hormone metabolites at the Erasmus medical centre, MercachemSyncom prepared a series of 13C6-labeled analogues of thyronine by a newly developed method with as key step a Chan-Lam coupling.
The synthesis of 13C6-labeled l-thyronine, 3,5-diiodothyronine, 3,3′,5-triiodothyroacetic acid and 3,3′,5,5′-tetraiodothyroacetic acid
Tetrahedron
2020 (76), 33, 131352

In collaboration with the ETH institute we have determined the operating conditions that lead to an efficient deracemization by temperature cycles.
Performance Analysis and Model-Free Design of Deracemization via Temperature Cycles
Org. Process Res. Dev. 2020

Together with Esteve Pharmaceuticals S.A., we invented compounds with a new dual mode of action to treat pain. These compounds show activity at α2δ of the voltage-gated calcium channels (VGCC), and the µ-opioid receptor (MOR).
New pyrrolidine-2-carboxylic acid derivatives for treating pain and pain related conditions
WO2020120606A1
WO2020120539A1

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