Lopchuk Lab

Today we report a mild transulfinamidation of alkyl and (hetero)aryl amines. This study was prompted by our need, across several medicinal chemistry programs, to generate sulfinamides, sulfonamides, and sulfonimidamides of complex pharmaceutical scaffolds at a late-stage.

Enjoyed spending time with @MoffittNews Drug Discovery team during our latest listening tour. It’s exciting to hear about the work underway to identify new cancer targets, develop promising small molecule therapies and move discoveries from the lab toward the clinic. @StuartMaudsley @monastyrskyi @LopchukLab @karenluMD #CancerResearch #CancerTherapeutics #TranslationalResearch

Preparation of Enantiopure Bifunctional S(VI) Transfer Reagent (t-BuSF) Submitting Authors: Zachary Shultz, Eve Hall, Prakash Warghude, Yun-Pu Chang, Justin M. Lopchuk Checking Authors: Taylor A. Stephens and Tehshik P. Yoon

nature.com/articles/s4155… nature.com/articles/s4146… Congratulations to Zachary Shultz, Eve Hall, Prakash Warghude, and Yun-Pu Chang. We are grateful to Taylor Stephens and Tehshik Yoon for their careful checking of our procedure.

The utility was further extended via an amine exchange process for the generation of highly complex S(VI) species. More work with this reagent is one the way, which will allow access to an ever increasing amount of sulfur chemical space.

Today in Organic Syntheses, we report the synthesis of t-BuSF, our enantiopure bifunctional S(VI) transfer reagent. orgsyn.org/demo.aspx?prep… It is used for the stereospecific preparation of sulfoximines, sulfonimidoyl fluorides, and sulfonimidamides.

Updates from the ChemRxiv version include a target-oriented synthesis of an oxadiazole fragment of an SK2 inhibitor. Congratulations to Daria and Vishala! pubs.acs.org/doi/10.1021/ac…

This method provides our first approach to acyl diaziridines, which we demonstrate as flexible intermediates readily converted to amides, hydrazides, acyl hydrazones and heterocycles.

Today in Org. Lett., we report the final version of our C-H amination of unactivated alkanes and aldehydes with diazirines via photocatalysis.

No metal catalyst or preactivation required. Congratulations to Connell and Zac. pubs.acs.org/doi/10.1021/ac…

The majority of available methods proved incompatible with such complexity, particular around solubility and numerous Lewis basic atoms. The chemistry is dump-and-stir, utilizing commercially-available alkyl amine salts or (hetero)aryl amines with Brønsted acids.

Today we report a mild transulfinamidation of alkyl and (hetero)aryl amines. This study was prompted by our need, across several medicinal chemistry programs, to generate sulfinamides, sulfonamides, and sulfonimidamides of complex pharmaceutical scaffolds at a late-stage.

Congratulations to Daria and Vishala! chemrxiv.org/doi/full/10.26…

Today in ChemRxiv, we report the C-H amination of unactivated alkanes and aldehydes with diazirines via photocatalysis. This method provides our first approach to acyl diaziridines, which are readily converted to amides, hydrazides, acyl hydrazones and heterocycles.

Today we’re celebrating the launch of @AccelerOnc, the first U.S. venture studio focused solely on oncology innovation and founded by Moffitt. By merging data, expertise and urgency, we’re driving bold ideas forward to prevent and cure cancer. #InnovationToImpact

Advance your career in #CancerResearch with the Moffitt Cancer PhD program! Application deadline: December 1, 2025 Are you passionate about fighting cancer? Our program prepares future scientists with a rigorous curriculum and offers four unique majors: • Cancer Biology • Cancer Chemical Biology • Cancer Immunology & Immunotherapy • Integrated Mathematical Oncology Why Moffitt? • Access to top research facilities • Collaborate with world-leading scientists • Hands-on experience in cutting-edge research • Supportive environment for innovation • Unmatched translational environment, turning discoveries into cures Start your journey to make a difference in cancer care and innovation. Learn more and apply now: bit.ly/3YH7yfH

The full job postings and application instructions are found below. The applications will be reviewed on a rolling basis until the positions are filled. …cancer-center-careers.hctsportals.com/jobs/2056785-p… …cancer-center-careers.hctsportals.com/jobs/2056980-p…

The second position focuses on the development of new chemistry for selective covalent inhibition. This encompasses method development, targeted synthesis, and translational collaborations. Applications are accepted by email at justin.lopchuk [at] moffitt [dot] org.

We have openings for two postdoc positions in synthetic organic chemistry. The first position focuses on the development of new chemical methods and reagents (with targeted synthesis applications) as well as a structure-based drug discovery program in oncology.

An offshoot of our S(VI) work, it allows for the rapid preparation of funtionalized phosphonates onto heterocycles. No transition metals or photochemistry required.

With the renewed interest in chemical methods around phosphonates, I thought it might be worth reposting a method we reported several years ago (especially since it seems people in the field have overlooked it...). arkat-usa.org/browse-arkivoc…