Regio- and Stereocontrolled-Synthesis of a Heterocycle
Fragment Collection Using Palladium Catalyzed C-H Arylation

Check out our latest work on from Sofia, Dani, Harry, Natalia and Matt on a C-H arylation approach to systematically access heterocycle fragments. / CEJ
doi.org/10.1002/chem...

Defluoroalkylation of Trifluoromethane with Organolithium Reagents: Mechanism and Synthesis of Fluoroalkenes We report a rare example of the transformation of HCF3 into a fluoroalkene functional group through defluoroalkylation. We rationalise product formation through DFT calculations, scale-up the synthes...

Hodan and Sarah's work in collaboration with @jamesabull.bsky.social and Phil Miller on transforming trifluoromethane (HFC-23) into fluoroalkenes is now out in @angewandtechemie.bsky.social here is the link: onlinelibrary.wiley.com/doi/10.1002/...

The stereochemistry of substitution at S(VI) Since the re-birth of sulfur-fluoride exchange (SuFEx) chemistry, coined by Sharpless in 2014 as a ‘click’ reaction, the prevalence of sulfur(vi) moieties in medicinal, polymer and materials chemistry...

📘 The stereochemistry of substitution at S(VI) ✨
by James A. Bull 𝘦𝘵 𝘢𝘭.

Insights into stereochemical outcomes in SuFEx & S(VI) substitution ⚗️🔄

#SulfurChemistry #Stereochemistry #ClickChem
🔗 doi.org/10.1039/D5QO01043H

Do Amino-Oxetanes Resemble Amides?
Check out our Matched Molecular Pairs study in
@chemrxiv.org comparing properties and structure.
Congrats @hikaruishikura.bsky.social and coworkers, in collaboration with Pfizer.
doi.org/10.26434/che...

As asymmetric sulfur(VI) derivatives become more prevalent in the chemical sciences, especially in aza-derivatives, sulfoximines, sulfonimidamides, we have reviewed "The stereochemistry of substitution at S(VI)"
doi.org/10.1039/D5QO...
with Ollie Symes, @orgchemfront.rsc.org

Synthesis of Cyclic Sulfilimines and Sulfoximines via Copper‐Mediated C(sp2)–H Sulfanylation of Benzylamines with a Catalytic Transient Directing Group Copper-mediated transient C─H sulfanylation of benzylamines with sulfenamides enables rapid access to thioethers, cyclic sulfilimines, and sulfoximines. Mechanistic investigations using 1H NMR and el....

Now published in ChemistryEurope: doi.org/10.1002/ceur...

SuFEx and SNAr on Sulfonimidoyl Fluorides - happy this is now published in ChemistryEurope.
chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/...
Catalytic SuFEx Reactivity of Sulfonimidoyl Fluorides with Functionalized Amines with Automation Applicable Conditions.
Congrats Nikki!

Happy to see our work on the divergent synthesis of difluorocyclobutanes, now published in #JOC: Synthesis of gem-Difluorocyclobutanes: Organolanthanum Enabled Synthesis and Divergent Catalytic Functionalization of gem-Difluorocyclobutanols. pubs.acs.org/doi/10.1021/... @hikaruishikura.bsky.social

Electrochemical Copper Catalysis: A Triple Catalytic System for Transient C(sp2)–H Functionalization Through Mediated Electrolysis | @ChemRxiv.
Congrats Freeman!
doi.org/10.26434/che...

Congrats to Freeman and Peerawat on our recent @ChemRxiv - Synthesis of Cyclic Sulfilimines and Sulfoximines via Copper Mediated C(sp2)–H Sulfanylation of Benzylamines with a Catalytic Transient Directing Group.
chemrxiv.org/engage/chemr...

Interested in strained rings or fluorine for medicinal chemistry - check out Hikaru’s work on difluorocyclobutanes on ChemRxiv.
doi.org/10.26434/che...

Catalytic SuFEx Reactivity of Sulfonimidoyl Fluorides with Functionalized Amines with Automation Applicable Conditions Sulfonimidamides have emerged as attractive chemical motifs in drug discovery and as sulfonamide bioisosteres that can offer improved pharmacokinetic and physiochemical properties. Here we report a mi...

Happy to report our work on catalytic SuFEx with sulfonimidoyl fluorides - and switchable SNAr reactions also. Congrats to Nikki on her paper now on ChemRxiv
doi.org/10.26434/che...

Development of automated workflows for direct-to-biology drug discovery of kinase inhibitors at Imperial College London on FindAPhD.com PhD Project - Development of automated workflows for direct-to-biology drug discovery of kinase inhibitors at Imperial College London, listed on FindAPhD.com

** PhD position ** We are advertising a chemical biology studentship with Vilar and Mann groups, and GSK with ICB CDT @icbcdt.bsky.social. #automation, #Synthesis, #direct-to-biology,
www.findaphd.com/phds/project...

🌟 Unlock Your Potential in Advanced Molecular Synthesis!
Gain skills and knowledge to excel in the dynamic field of molecular synthesis.
🔗 Apply Today! www.imperial.ac.uk/study/course...

#Chemistry #MolecularSynthesis #ImperialCollege #Research #Innovation #PostgraduateStudies #MRes #Research

How to thrive at conferences Five tips for making the most of meet-ups

🌟 Alumni Spotlight: Rupali Dabas 🌟 Celebrating the achievements of our MRes in Drug Discovery & Development alumni! Her article is in @chemistryworld.com on conferences. 🌍✨ 🔗 Read more: www.chemistryworld.com/careers/how-... #AlumniImpact #ChemistryCommunity #ImperialCollegeLondon #DrugDiscovery

New dimensions for covalent enantioprobe chemoproteomics at Imperial College London on FindAPhD.com PhD Project - New dimensions for covalent enantioprobe chemoproteomics at Imperial College London, listed on FindAPhD.com

We are advertising a 2nd fully funded PhD studentship with Ed Tate and ICB CDT for October:
New dimensions for covalent enantioprobe chemoproteomics
#chemicalbiology, #synthesis, #chemoproteomics, #CHfunctionalisation.
www.findaphd.com/phds/project...

Studentships for October 2025 entry 2025 Studentship Opportunities

We are advertising an exciting PhD studentship related to covalent drug discovery with Tate, Armstrong & Mann groups and Vertex pharmaceuticals with ICB CDT.
"Warheads take the strain in chemoproteomics"
#Synthesis, #Strained_rings, #Chemoproteomics
Apply here: www.imperial.ac.uk/chemical-bio...

Description Please note that job descriptions are not exhaustive, and you may be asked to take on additional duties that align with the key responsibilities ment...

We are recruiting for a postdoctoral Research Associate in Synthetic Chemistry to work in C-H functionalisation. Come join us Imperial! @imperialchemistry.bsky.social
3-year position. Closing: 19-March-2025. shorturl.at/uwERp
#Chempostdoc, #CHfunctionalization, #Heterocycles

Thanks so much to @jamesabull.bsky.social and team for this great review, online now and #OpenAccess! @imperialchemistry.bsky.social

The RSC Organic Chemistry Community South-East Regional Meeting will be hosted by Imperial Chemistry
@imperialchemistry.bsky.social on Friday 28th March 2025 with an excellent speaker line-up. For more details, to register, & submit poster abstract (PhD/PDRAs), see here: www.rsc.org/events/detai...

Unconventional reactivity of sulfonyl fluorides Sulfonyl fluorides are now established click reagents that find broad applications in synthesis, chemical biology, and drug discovery. Sulfonyl fluori…

We have reviewed the emerging "Unconventional reactivity of sulfonyl fluorides", here: www.sciencedirect.com/science/arti...

Celebrating Christmas with a new cover design inspired by @jamesabull.bsky.social's team and their work on sulfoximine-bicyclo[1.1.0]butanes. These warheads are a game-changer for protein research with their tuneable reactivity!

#sciart ⌬ #research ⌬ #chemistry

Bull Group at table ahead of a meal on a lab Christmas party

Good times at the group Christmas party

Harnessing Oxetane and Azetidine Sulfonyl Fluorides for Opportunities in Drug Discovery Four-membered heterocycles such as oxetanes and azetidines represent attractive and emergent design options in medicinal chemistry due to their small and polar nature and potential to significantly impact the physiochemical properties of drug molecules. The challenging preparation of these derivatives, especially in a divergent manner, has severely limited their combination with other medicinally and biologically important groups. Consequently, there is a substantial demand for mild and effective synthetic strategies to access new oxetane and azetidine derivatives and molecular scaffolds. Here, we report the development and use of oxetane sulfonyl fluorides (OSFs) and azetidine sulfonyl fluorides (ASFs), which behave as precursors to carbocations in an unusual defluorosulfonylation reaction pathway (deFS). The small-ring sulfonyl fluorides are activated under mild thermal conditions (60 °C), and the generated reactive intermediates couple with a broad range of nucleophiles. Oxetane and azetidine heterocyclic, -sulfoximine, and -phosphonate derivatives are prepared, several of which do not have comparable carbonyl analogs, providing new chemical motifs and design elements for drug discovery. Alternatively, a SuFEx pathway under anionic conditions accesses oxetane-sulfur(VI) derivatives. We demonstrate the synthetic utility of novel OSF and ASF reagents through the synthesis of 11 drug analogs, showcasing their potential for subsequent diversification and facile inclusion into medicinal chemistry programs. Moreover, we propose the application of the OSF and ASF reagents as linker motifs and demonstrate the incorporation of pendant groups suitable for common conjugation reactions. Productive deFS reactions with E3 ligase recruiters such as pomalidomide and related derivatives provide new degrader motifs and potential PROTAC linkers.

Very happy to use my first post here to say thanks and congratulations to the team for their great work on our latest study on oxetanes and azetidines, out now in JACS. doi.org/10.1021/jacs...