This enantioselective nucleophilic CH fluorination was finally realized in collaboration with BMS colleagues, what a fantastic collaboration!.

The goal was initially set via a collaboration with Pfizer, 18 years is too long a wait, but that is science.

First challenge from the legend Lerner when I arrived at Scripps in 2007 summer was CH fluorination with 18F. Finally, we have realized the first example and added enantioselectivity on top, Nature Catal: Again, bifunctional Liand is the key!

It is also a great way to oxidize beta and gamma CH with just TBHP oxidant.

One Ligand three CH birds. Temporal control is key for activating three CH on different sites, just like symphony, otherwise will be a mess instead of structure oriented CH reaction:

We had two ideas to close catalytic cycle for CH activation in 2001: one is CH oxidation with peroxides via Pd(IV) (Koten, Canty); one is CH coupling with RB via Pd(0) (Suzuki). Overwhelmed to be connected to the legend this way….

RT @NSF: Today, NSF announced an add’l 500 NSF Graduate Research Fellowship Program awardees for the 2025-2026 cohort, bringing the total t….

Weak coordination is very powerful with the help from bifunctional ligands; making secondary alkyl-fluoride building blocks from diverse simple substrates is highly valuable in drug discovery:

Enantioselective CH activation is still on gas pedal. for broad applications, we must develop new catalysts for reacting CH with nucleophiles: What is your wish list? NaF? NaCl? H2O? NH3?

A high bar for CH reactions to be relevant for sustainable polymer synthesis. Incredible efforts from a Germany Tech Institute to improve and pressure test one of our C-H reaction towards industrialization, even solvent needs to be omitted: just soap in and gold out!

EnantioCH by our MPAA ligand fills a gap in chiral technology; creating new chemical space for both drug discovery and chiral ligands:

New chemical space in drug discovery means positioning H-A, H-D, pi-interactions, etc within various distal and geometric relationships at angstrom precision. CH activation at different sites have now arrived in large quantities to do just that:

First in class pain killer FDA approved: Great fun memories working with Vertex on CH editing of this THF, THP scaffolds. 80 M patients annually could benefit

A magic spoon of table salts for aliphatic acids in 2007 guided us along the path of CH activation based on weak coordination, leading to discoveries of 10 distinct classes of bifunctional ligands so far, but ketones are too slippery until now: Nature: 10.1038/s41586-024-08281-4

RT @filippo_romiti: EJ: the man, the myth, the legend.

Design of chiral bifunctional ligands Continues to expand the scope of enantio-CH activation reactions, even when FG and CH are out of plane. Next will be ketone to conquer….

RT @scrippsresearch: Today marks a monumental milestone: 100 years of pioneering science at Scripps Research. 🎉 On December 11, 1924, phila….

Wonderful host. Great talks from @engle lab, @Giri_Research and collaborators from BMS and Vividion. Chemistry really matters in drug discovery.

Amazing collaboration with Stoltz group @Caltech and Davies group @EmoryUniversity! Our part was to achieve tetra-CH hydroxylation via weak coordination at very late stage of complex total synthesis:.

CH Lactonization is a way for oxidation. we have done beta lactone, now gamma lactones. Controlling site-selectivity between CH3 and CH2 by catalyst is really challenging: