Jon Ellman

About

Jon Ellman is the Eugene Higgins Professor of Chemistry and Professor of Pharmacology at Yale University, and has been a member of the Yale faculty since 2010. His research focuses on the rapid and efficient synthesis of new chemical matter, aiming to discover and develop compounds with diverse properties and applications. His laboratory has pioneered the development of tert-butanesulfinamide chemistry, which is extensively used for the asymmetric synthesis of amine-containing compounds prevalent in pharmaceuticals. Additionally, his work involves the catalytic conversion of C-H to C-C bonds, enabling the direct preparation of complex structures from simple precursors. Ellman's research also includes designing and synthesizing structures that interact with biological systems, developing tools to understand enzyme function, and creating compounds to interact with biomolecular targets for potential drug development.

Research topics

• Chemistry
• Stereochemistry
• Organic chemistry
• Biology
• Biophysics
• Medicine
• Combinatorial chemistry
• Photochemistry
• Computational biology
• Computational chemistry

Selected publications

• Bespoke library docking for 5-HT2A receptor agonists with antidepressant activity

  Nature · 2022 · 248 citations

  Senior authorCorresponding
  DOI

• Catalytic Enantioselective Sulfur Alkylation of Sulfenamides for the Asymmetric Synthesis of Sulfoximines

  Journal of the American Chemical Society · 2022 · 152 citations

  Senior authorCorresponding

  -alkylation products were efficiently converted to a variety of sulfoximines with complete retention of stereochemistry. The utility of this approach was further demonstrated by the asymmetric synthesis of a complex sulfoximine agrochemical.

  DOI

• Highly Diastereoselective Functionalization of Piperidines by Photoredox-Catalyzed α-Amino C–H Arylation and Epimerization

  Journal of the American Chemical Society · 2020 · 82 citations

  Senior authorCorresponding

  oxidation. Following the rapid and unselective C-H arylation reaction, a slower epimerization occurs to provide the high diastereomer ratio observed for a majority of the products. Several stereoisomerically pure products were resubjected to the reaction conditions, each of which converged to the experimentally observed diastereomer ratios. The observed distribution of diastereomers corresponds to a thermodynamic ratio of isomers based upon their calculated relative energies using density functi…

  DOI

• Sulfur-Arylation of Sulfenamides via Ullmann-Type Coupling with (Hetero)aryl Iodides

  Organic Letters · 2023-06-20 · 61 citations

  articleOpen accessSenior authorCorresponding

  Sulfur-(hetero)arylation of sulfenamides with commercially abundant (hetero)aryl iodides by Ullmann-type coupling with inexpensive copper(I) iodide as the catalyst is reported. A broad scope of reaction inputs was demonstrated, including both aryl and alkyl sulfenamides and highly sterically hindered aryl and 5- and 6-membered ring heteroaryl iodides. Relevant to many bioactive high oxidation state sulfur compounds, the (hetero)arylation of S-methyl sulfenamides is reported, including for comple…

  PublisherOA PDFDOI

• Enantioselective <i>S</i>‐Alkylation of Sulfenamides by Phase‐Transfer Catalysis

  Angewandte Chemie International Edition · 2024-07-26 · 44 citations

  articleOpen accessSenior authorCorresponding

  A general phase-transfer catalyst (PTC) mediated enantioselective alkylation of N-acylsulfenamides is reported. Essential to achieving high selectivity was the use of the triethylacetyl sulfenamide protecting group along with aqueous KOH as the base under biphasic aqueous conditions to enable the reaction to be performed at -40 °C. With these key parameters, enantiomeric ratios up to 97.5 : 2.5 at the newly generated chiral sulfur center were achieved with an inexpensive cinchona alkaloid derive…

  PublisherOA PDFDOI

Recent grants

• Application of Sulfinamides in Synthesis and Catalysis

  NSF · $480k · 2011–2014

• NIH Grant U19CA053617

  NIH · $6.7M · 2002

• Asymmetric Synthesis Using tert-Butanesulfinamide

  NSF · $390k · 2005–2008

Frequent coauthors

• Robert G. Bergman

  Lawrence Berkeley National Laboratory

  252 shared

• Bruce H. Lipshutz

  University of California, Santa Barbara

  75 shared

• Nicholas E. Leadbeater

  University of Connecticut

  75 shared

• Brandon Q. Mercado

  Yale University

  66 shared

• Margaret M. Faul

  Washington University in St. Louis

  65 shared

• Mark Lautens

  65 shared

• Brianna Lucas

  University of Florida

  64 shared

• Julia B. Scheerer

  William & Mary

  64 shared

Labs

• Ellman LaboratoryPI

Education

• National Science Foundation Postdoctoral Fellow, Department of Chemistry

  University of California, Berkeley

  1992

• Ph.D., Department of Chemistry

  Harvard University

  1989

• B.S., Department of Chemistry

  Massachusetts Institute of Technology

  1984

Awards & honors

• NSF Predoctoral Fellowship (1984)
• NSF Postdoctoral Fellowship (1989)
• NSF Young Investigator Award (1993)
• Arnold and Mabel Beckman Foundation Young Investigator Award…
• Burroughs Wellcome Fund Hitchings Award for Drug Design and…

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