#Halogenation
This is such a neat idea from the @narayanlab.bsky.social and the @hartwiggroup.bsky.social now in #JACSasap fooling enzymes with a removable binding ligand to accept non-native substrates #ChemSky
Site-, Stereo-, and Chemoselective Enzymatic Halogenation of Terpenoids by a Substrate Masquerade
Enzymatic halogenation of C–H bonds is a promising approach to synthesize chlorine-containing compounds. However, few halogenases chlorinate C(sp3)–H bonds of molecules lacking a carrier protein, and ...
pubs.acs.org
September 27, 2025 at 6:24 PM
Microbially-mediated halogenation and dehalogenation cycling of organohalides in the ocean www.biorxiv.org/content/10.1... #jcampubs 🌊
May 22, 2025 at 1:58 PM
Now online:

Article by Ning Jiao, Song Song & co-workers

Direct regioselective C-3 halogenation of pyridines

www.nature.com/articles/s44... ($)
#Chemsky
Direct regioselective C-3 halogenation of pyridines - Nature Synthesis
Direct regioselective C-3 halogenation of pyridines is achieved using ether solvents, and interactions between the pyridine substrate, ether solvent and haleniums play a dominant role in the reactivit...
www.nature.com
November 5, 2025 at 12:20 PM
www.organic-chemistry.org/abstracts/li...
A mechanoredox system using ball milling to activate piezoelectric BaTiO3 enables solvent-minimized, metal-catalyst-free halogenation of aryl diazonium salts under air.
September 28, 2026 at 6:30 PM
Chicken chemistry 101 a halogenation reactions. #chemsky
August 13, 2025 at 10:40 PM
Excited that our paper on enzymatic bromination of peptides is now online at ACS Chemical Biology! Led by Haley Bridge, we showed that the flavin-dependent halogenase RebH and its variants can be used for late-stage chemoenzymatic diversification of bioactive peptides: pubs.acs.org/doi/10.1021/...
Enzymatic Bromination of Native Peptides for Late-Stage Structural Diversification via Suzuki–Miyaura Coupling
Flavin-dependent halogenases (FDHs) provide a biocatalytic approach for the site-selective halogenation of aromatic compounds, but their use in late-stage functionalization of peptides has remained li...
pubs.acs.org
April 28, 2026 at 2:36 PM
Crystal structures of AetF in complex with tryptoline and 8-bromotryptoline reveal the structural basis of regioselective halogenation and suggest two potential pathways to the formation of 6,8-dibromotryptoline #TryptophanHalogenases #Bromination doi.org/10.1107/S205...
September 21, 2026 at 1:45 PM
📣 New Publication 🧪

📄 H2-Driven Flavin Recycling Supports Biocatalytic Halogenation by Flavin-Dependent Halogenase

🔗 Read it here: doi.org/10.1002/cctc...
📲 View SCHEMA research: schemahub.web.ox.ac.uk/publications

#Biocatalysis #Flavin #Halogenation #Chemistry

@chemistryeurope.bsky.social
December 15, 2025 at 8:36 AM
Now online:

News & Views on the Articles:

www.nature.com/articles/s44... ($)

And

www.nature.com/articles/s44... ($)

meta-Selective radical halogenation of pyridines by Nirmala Mohanta & Jacquelyne A. Read

www.nature.com/articles/s44... ($)
#Chemsky
meta-Selective radical halogenation of pyridines - Nature Synthesis
Radical processes can be leveraged to impart meta selectivity in pyridine functionalization, offering a valuable approach for the late-stage functionalization of bioactive molecules.
www.nature.com
January 5, 2026 at 12:44 PM
De novo biosynthesis of halogenated benzoxazinoids in Nicotiana benthamiana www.sciencedirect.com/science/arti...
De novo biosynthesis of halogenated benzoxazinoids in Nicotiana benthamiana
Halogenation of natural products can improve their bioactivity, pharmacokinetics, and commercial value, yet sustainable production of halogenated smal…
www.sciencedirect.com
April 21, 2026 at 3:41 PM
Now online:

Article by Xiaotian Qi, Qiang Cheng & co-workers

Spin-density-controlled radical coupling for meta-selective C–H halogenation of pyridines

www.nature.com/articles/s44... ($)
#Chemsky
Spin-density-controlled radical coupling for meta-selective C–H halogenation of pyridines - Nature Synthesis
In this study meta-selective single-step bromination and chlorination reactions of pyridines and their derivatives are developed, with pyridinium radical cations as the key intermediates. A spin-densi...
www.nature.com
September 2, 2025 at 1:38 PM
Separation of halide oxidation and substrate halogenation chemistries rationalizes site-selective vanadium dependent haloperoxidase catalysis www.biorxiv.org/content/10.1101/2025.10.24.684477v1 #cryoem
October 26, 2025 at 11:46 AM
What happens if you substitute all protons by halogens in a photoactive complex?
In our new publication, we show how ligand perhalogenation reshapes redox & photophysical properties in Ni(0) complexes.
@wengeroliver.bsky.social in cooperation with Malischeski-group
doi.org/10.1021/acs....
Controlling Redox and Photophysical Properties of First-Row Transition Metal Complexes via Ligand Perhalogenation
Halogenation of ligands intensely modulates the redox and photophysical properties of transition-metal complexes, yet fully halogenated systems remain largely unexplored. Here we report the synthesis ...
doi.org
March 2, 2026 at 8:22 AM
A binuclear copper enzyme platform for enantioconvergent radical (pseudo)halogenation https://www.biorxiv.org/content/10.64898/2026.09.20.753013v1
September 22, 2026 at 3:45 PM
Great start into 2025!!! Thanks to the #VHPO Team in the Gulder lab. Check out our latest report on how employing enzymes in cascade reactions.

pubs.acs.org/doi/10.1021/...
Chemoenzymatic C,C-Bond Forming Cascades by Cryptic Vanadium Haloperoxidase Catalyzed Bromination
Inspired by natural cryptic halogenation in C,C-bond formation, this study developed a synthetic approach combining biocatalytic bromination with transition-metal-catalyzed cross-coupling. Using the c...
pubs.acs.org
January 3, 2025 at 8:01 PM
A binuclear copper enzyme platform for enantioconvergent radical (pseudo)halogenation https://www.biorxiv.org/content/10.64898/2026.09.20.753013v1
September 22, 2026 at 3:45 PM
Ben Millwater (Cohort 10) recently attended the European Peptide Symposium in Vienna 🇦🇹.
Ben successfully presented his PhD research on the regioselective halogenation of tryptophan-containing peptides and non-native aromatic substrates.
Many thanks to the organisers and Ben's supervisory team!
September 17, 2026 at 8:16 AM
What is responsible for the halogen specificity & is there a Substrate binding Site in #VHPOs? Learn more about this amazing enzyme class in our latest paper @naturecomms.bsky.social Congratulations to the Team! www.nature.com/articles/s41...
Unraveling the molecular basis of substrate specificity and halogen activation in vanadium-dependent haloperoxidases - Nature Communications
Vanadium-dependent haloperoxidases (VHPOs) are versatile enzymes that catalyze oxidation of halides followed by halogenation of electron-rich substrates, but the factors dictating substrate and haloge...
www.nature.com
March 2, 2025 at 8:34 PM
Cryptic halogenation and cyclopropanation for the biosynthesis of a new noncanonical amino acid. Very cool.

www.biorxiv.org/content/10.1...
Biosynthesis of Strained Amino Acids Through a PLP-Dependent Enzyme via Cryptic Halogenation
bioRxiv - the preprint server for biology, operated by Cold Spring Harbor Laboratory, a research and educational institution
www.biorxiv.org
December 16, 2023 at 1:57 AM
Copper-dependent halogenases supercharge C-H bond functionalization, achieving selectivity in organic synthesis. Unveil C(sp³)-H halogenation magic! #ChemRevolution PMID:39880944, Nature 2025, @Nature https://doi.org/10.1038/s41586-024-08362-4 #Medsky #Pharmsky #RNA #ASHG #ESHG 🧪
Copper-dependent halogenase catalyses unactivated C−H bond functionalization | Nature
Carbon–hydrogen (C–H) bonds are the foundation of essentially every organic molecule, making them an ideal place to do chemical synthesis. The key challenge is achieving selectivity for one particular C(sp3)−H bond1–3. In recent years, metalloenzymes have been found to perform C(sp3)−H bond functionalization4,5. Despite substantial progresses in the past two decades6,7, enzymatic halogenation and pseudohalogenation of unactivated C(sp3)−H—providing a functional handle for further modification—have been achieved with only non-haem iron/α-ketoglutarate-dependent halogenases, and are therefore limited by the chemistry possible with these enzymes8. Here we report the discovery and characterization of a previously unknown halogenase ApnU, part of a protein family containing domain of unknown function 3328 (DUF3328). ApnU uses copper in its active site to catalyse iterative chlorinations on multiple unactivated C(sp3)−H bonds. By taking advantage of the softer copper centre, we demonstrate t
doi.org
April 8, 2025 at 6:50 AM
You'd think we would've learned to leave halogenation as a last resort by now
January 7, 2025 at 2:45 PM