Dan Priebbenow

Just published online at Chemical Science, our group's most recent work on "Visible-Light Induced Click Reactions of Acylsilanes with Pyruvate Electrophiles" - led by Final Year PhD student Rowan with help from the Braese Group in Karlsruhe doi.org/10.1039/D5SC...

Just published online at JACS, our group's most recent work on "Distal C(sp3)-H Amidation via Ind*RhIII Catalyzed Nitrene Transfer" - led by 2nd Year PhD student Hannah. pubs.acs.org/doi/full/10....

Discovery of WEE1 Kinase Inhibitors with Potent Activity against Patient-Derived, Metastatic Colorectal Cancer Organoids A library of potent WEE1 kinase inhibitors was synthesized based on the discontinued frontrunner clinical candidate AZD1775 (1), many of which were more selective for WEE1 over an undesirable off-target of 1, the kinase PLK1. When tested against patient-derived organoids (PDOs) grown from TP53-mutated colorectal cancer (CRC) peritoneal metastases, 34 (IC50 value of 62 nM) exhibited stronger efficacy than 1 (IC50 value of 120 nM) and the best-in-class clinical candidate ZN-c3 (IC50 value of 127 nM). Against primary CRC PDOs with TP53-WT, 34 significantly enhanced DNA damage, replication stress and apoptosis compared to 1, as well as demonstrated high selectivity over patient-matched normal healthy colon PDOs, highlighting a potential therapeutic window for cancer treatment. Overall, this investigation provides critical insight into several potent WEE1 inhibitors that exhibited exceptional efficacy against CRC PDOs and is the first to utilize a PDO platform to assess their effect on healthy and malignant cell viability.

Led by final year PhD student Joel, this article detailing the "Discovery of WEE1 Kinase Inhibitors with Potent Activity against Patient-Derived, Metastatic Colorectal Cancer Organoids" was recently published in the Journal of Medicinal Chemistry pubs.acs.org/doi/abs/10.1...

Acylsilanes as Weakly Coordinating Directing Groups for Metal-Catalyzed C–H Functionalization The capacity to engage acylsilanes as carbene precursors, electrophiles, and acyl radical precursors offers significant synthetic potential. However, harnessing the versatility of acylsilanes in chemi...

Our review covering recent advances in the use of "Acylsilanes as Weakly Coordinating Directing Groups for Metal-Catalyzed C–H Functionalization" was recently published ACS Catalysis - led by 3rd year PhD student Rowan pubs.acs.org/doi/abs/10.1...

A postdoctoral position, funded by the Leverhulme Trust for up to 36 months, is available to join my group at the University of Edinburgh. The project focuses on biomimetic approaches to natural product synthesis.

Deadline: 18th April 2025.

elxw.fa.em3.oraclecloud.com/hcmUI/Candid...

Our group’s latest project is now online at ChemRxiv involving the reaction of Visible-Light Induced Carbenes with Pyruvate Electrophiles #Chemsky chemrxiv.org/engage/chemr...

🚨Just 2 weeks from today! On Jan 15 - the first session of the 2025 season of the ACS DOC @organicdivision.org Virtual Symposium
Free to watch live at the links below

#Chemsky

#Chemsky #Science

The Synthesis of Sulfonyl Fluoride Functionalized 2-Aminothiazoles Using a Diversity Oriented Clicking Strategy We present a Diversity Oriented Clicking approach to synthesize a library of novel clickable N-substituted 2-aminothiazoles which serve as versatile hubs for SuFEx click chemistry diversification. Lev...

Happy to have contributed to this work out of MIPS led by Chris Smedley on a Diversity Oriented Click Strategy to access SO2F-thiazoles
pubs.acs.org/doi/10.1021/...

Distal C(sp3)-H Amidation via Ind*RhIII Catalysed Nitrene Transfer using 1,4,2-Dioxazol-5-ones

Authors: Hannah Ross, Yihui Yu, Liselle Atkin, Daniel Priebbenow
DOI: 10.26434/chemrxiv-2024-m5xps

Distal C(sp3)-H Amidation via Ind*RhIII Catalysed Nitrene Transfer using 1,4,2-Dioxazol-5-ones Building on our discovery that Ind*Rh(III) catalysts accelerated C(sp2)–H amidation, the Ind*Rh(III) catalysed amidation of C(sp3)–H sites was explored harnessing amides as weakly-coordinating directi...

Our groups latest work exploring the Rh-catalysed amidation of C(sp3)-H bonds is now online at ChemRxiv

chemrxiv.org/engage/chemr...

Distal C(sp3)-H Amidation via Ind*RhIII Catalysed Nitrene Transfer using 1,4,2-Dioxazol-5-ones Building on our discovery that Ind*Rh(III) catalysts accelerated C(sp2)–H amidation, the Ind*Rh(III) catalysed amidation of C(sp3)–H sites was explored harnessing amides as weakly-coordinating directi...

Our groups latest work exploring the Rh-catalysed amidation of C(sp3)-H bonds is now online at ChemRxiv

chemrxiv.org/engage/chemr...

We are hiring (resharing appreciated)!

Given recent successful grant applications (I got my SNSF Starting Grant 🚀), we are extending the LIAC team with multiple openings (PhD/postdoc) for 2025.

Apply now (deadline: December 20th) by filling in this form: forms.fillout.com/t/eq5ADAw3kkus.
#ChemSky

Chemdle Curated daily chemistry problems. Six attempts to solve the questions, on topics from named reactions to total synthesis.

Synthetic chemists! If you haven’t discovered chemdle yet, you are missing out big time! Synthesis meets wordle!

www.chemdle.com

Might seem like a trivial change but the PhB(neop) has worked better for us than PhB(pin)

Thanks for coming to visit us down under - was great to meet you all!

Benzocyclobutenone synthesis exploiting acylsilanes as photofunctional directing groups The visible-light irradiation of acylsilane tethered vinyl ketones promotes an intramolecular Stetter-type reaction via siloxycarbene intermediates. To exploit this unique mode of reactivity, we herei...

From triangles to squares: building on our previous studies into photochemical cyclopropanation, our latest work on the photochemical cyclisation of acylsilanes to generate benzocyclobutenone scaffolds is now online. Check it out: pubs.rsc.org/en/content/a...