Nik Chekshin, PhD

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Nik Chekshin, PhD

Nik Chekshin, PhD

@NikChekshin

Medicinal Chemistry | Computer-Accelerated Drug Discovery

La Jolla, California انضم Ekim 2016
409 يتبع212 المتابعون
Nik Chekshin, PhD
Nik Chekshin, PhD@NikChekshin·
A long-chased dream reaction, enantioselective nucleophilic C-H fluorination is unlocked by our ligand design under Pd catalysis, enabling rapid diversification of drug-like molecules and radiolabelling for PET. Huge thanks to @scrippsresearch and @bmsnews for continuous support!
Scripps Research@scrippsresearch

The @YulabJin reports a one-step method to stereoselectively attach fluorine to drug-like molecules using low-cost fluoride. Published in @NatureCatalysis with first author @NikChekshin and @bmsnews, the approach uses fluorine-18 for PET imaging to track bioactive compounds and accelerate drug discovery. More: ow.ly/kttg50XHyPg

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Nik Chekshin, PhD أُعيد تغريده
Scripps Research Graduate Program
Scripps Research Graduate Program@ScrippsGradPrgm·
In the @YulabJin, @NikChekshin discovered & developed novel catalytic systems for selective C-H functionalization, unlocking access to new chemical space & enabling synthesis of structurally diverse libraries of bioactive molecules & medicinal targets.💻: scripps.edu/graduation.
Scripps Research Graduate Program tweet media
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Nik Chekshin, PhD
Nik Chekshin, PhD@NikChekshin·
One of the most memorable moments of my PhD was the discovery of exceptional stereocontrol of MPASA ligands in asymmetric incorporation of nucleophiles into C(sp3)–H bonds. Excited to see first application published as the Editor's Choice Article @J_A_C_S pubs.acs.org/doi/10.1021/ja…
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Nik Chekshin, PhD
Nik Chekshin, PhD@NikChekshin·
Our new breakthrough is out in @Nature! Our ligand design for a cationic catalyst assembly unlocked C–H coupling, arylation, and oxidation of ketones and esters. Congratulations to my collaborator Yi-Hao Li for driving this work with exemplary efficiency! nature.com/articles/s4158…
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Nik Chekshin, PhD أُعيد تغريده
Scripps Research
Scripps Research@scrippsresearch·
Today marks a monumental milestone: 100 years of pioneering science at Scripps Research. 🎉 On December 11, 1924, philanthropist and journalist Ellen Browning Scripps laid the foundation for what would become a globally renowned institute. Learn more at 100.scripps.edu.
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Nik Chekshin, PhD
Nik Chekshin, PhD@NikChekshin·
Honoured to receive the JM Award from IPMI! I'm most thankful to my doctoral advisor Prof. Jin-Quan Yu and to Scripps Research for the tremendous support and the unparalleled opportunities to advance the frontiers of catalysis and work with the most brilliant minds in the field.
Scripps Research@scrippsresearch

Congrats to doctoral researcher @NikChekshin on receiving the 2024 @PreciousIPMI @Johnson_Matthey Award for his work in Pd-catalyzed C-H functionalization—a method advancing sustainable practices in medicinal and materials chemistry. More: ow.ly/zWaB50TIeGS

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Nik Chekshin, PhD
Nik Chekshin, PhD@NikChekshin·
We broke 4 C-H bonds at once! This enantioselective cascade combines our earlier work on free acid dehydrogenation producing a norbornene equivalent in situ with Catellani-type polyarylation to construct 4 C-C bonds and 3 new stereosenters in a single step doi.org/10.1002/anie.2…
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Nik Chekshin, PhD أُعيد تغريده
Yulab
Yulab@YulabJin·
Yamada-Koga asymmetric lithiation is part of the inspiration for our first project on asymmetric CH palladation in 2002. This recognition is so special to my coworkers: CH activation is finally a significant member of the asymmetric catalysis family, huge potential to yet improve
Yulab tweet mediaYulab tweet mediaYulab tweet mediaYulab tweet media
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Nik Chekshin, PhD
Nik Chekshin, PhD@NikChekshin·
In our new report, we discovered a dual-ligand system to overcome the intrinsic electronic bias in the olefination of protected phenols without directing templates - our ligand design controlled site-selectivity by altering reversibility of C-H palladation.pubs.acs.org/doi/10.1021/ac…
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Nik Chekshin, PhD أُعيد تغريده
Yulab
Yulab@YulabJin·
Since Enantioselective beta C-H activation in 2016, we have chased gamma and delta relentlessly, finally: science.org/doi/epdf/10.11…
Yulab tweet media
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Nik Chekshin, PhD
Nik Chekshin, PhD@NikChekshin·
We have now utilized the power of ligand control to achieve regioselectivity in β,γ-dehydrogenation of free carboxylic acids, providing a versatile platform for the downstream functionalization of complex molecules at remote γ-sites. pubs.acs.org/doi/10.1021/ja…
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Nik Chekshin, PhD أُعيد تغريده
Yulab
Yulab@YulabJin·
Breath taking efforts from Pharma to find selective inhibitor for Sodium channels. Our CH editing of THF and THP scaffold in 2015 finds the the THF lead (vertex collaboration with Dean Stamos)optimized to give 30k fold selectivity. Medicine for acute pain, very much needed.
Yulab tweet media
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Nik Chekshin, PhD
Nik Chekshin, PhD@NikChekshin·
@mx_million Excellent overview! I remember looking for a thorough practical comparison and can't imagine it done better, congratulations Max and the rest of the team!
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Max Palkowitz
Max Palkowitz@mx_million·
Echem or Photochem? The age old question. Very excited to share this guide to navigating these two technologies! In here you will find side-by-side mechanisms, scope analyses, and a synthesis guide for many electro- and photochemical reactions! chemrxiv.org/engage/chemrxi…
Max Palkowitz tweet media
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Nik Chekshin, PhD
Nik Chekshin, PhD@NikChekshin·
Our paper now in @acsJACS shows how ligand design enabled bromination of acids, featuring enzyme-inspired H-bonding mediated substrate anchoring via a proposed macrocyclic TS assembly. Congratulations to the entire Scripps team and all our collaborators! pubs.acs.org/doi/10.1021/ja…
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Nik Chekshin, PhD
Nik Chekshin, PhD@NikChekshin·
With continuous molecular design of catalytic templates, we've now extended the power of precise structural editing and demonstrated regiocontrol in remote olefination of heterobiaryls. Excited to see this work published, congratulations to the entire team!onlinelibrary.wiley.com/doi/10.1002/an…
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Nik Chekshin, PhD
Nik Chekshin, PhD@NikChekshin·
Excited to have helped overcome long-standing issues of poor reactivity and substrate inhibition in unlocking the C-H functionalization of heteroarenes under Pd catalysis by designing a dual-catalyst system to tune Pd character. Congratulations to our team pubs.acs.org/doi/full/10.10…
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