I am proud to share our work in #JMedChem for one-pot #PROTAC synthesis via photochemical C(sp2)-C(sp3) cross coupling and amide bond formation. In the paper you can find comprehensive scopes detailing the substrate tolerance of the photochemical C(sp2)-C(sp3) coupling on various CRBN binders and linker motifs. The one-pot synthesis grants rapid access to BRD4 PROTACs in a single step via heterobifunctinal linker building blocks. This might be useful to #MedChemists looking to overcome the synthetic hurdles of making a lot of #PROTACs fast for #drug discovery programs. You can read about our work in #JMedChem here: https://lnkd.in/eyCiE3HG and can find some nice illustrations of our #PROTAC factory on the cover of J. Med. Chem. as well. This project was a great collaborative effort between Boehringer Ingelheim and the University of Mainz. Many thanks to Christine Marie Arndt, Jacqueline Bitai, Jessica Brunner, Till Opatz, Paola Martinelli, Andreas Gollner and Kevin Sokol. Special thanks to Harald Weinstabl for funding these wild ideas that eventually turn into something useful for the daily work in drug discovery.
Pleasure and honor to be part of this. More ideas in the pipeline! Best wishes to all of you & A Happy New Year!
Pleasure to support such a great collaborative effort of industry Matthias Krumb, Kevin Sokol, Andreas Gollner, Jacqueline Bitai, Paola Martinelli and academia Till Opatz, Christine Marie Arndt
Great work. Congratulations.
Amazing!
Great work and awesome cover!
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7moMatthias, thanks you for sharing! . Much appreciated!