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E. J. Corey

E. J. Corey

· Sheldon Emory Professor EmVerified

Harvard University · Chemistry and Chemical Biology

Active 1950–2026

h-index150
Citations101.3k
Papers1.5k10 last 5y
Funding
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About

Elias J. Corey is the Sheldon Emory Professor Emeritus whose research group focuses on various areas of experimental chemistry, including multi-step, mechanistic, and exploratory synthesis. His work encompasses the development and application of synthetic methods to construct complex molecules. Corey has authored several influential books, such as "The Logic of Chemical Synthesis," "Molecules and Medicine," and "Enantioselective Chemical Synthesis." The latter book provides a comprehensive and concise presentation of the most useful enantioselective processes available to synthetic chemists, discusses logical approaches to applying these methods in the synthesis of stereochemically complex molecules, and details numerous reaction sequences used to build a wide variety of complex target molecules. Over his career, Corey has published more than 1000 scientific papers between 1948 and 2010, reflecting his extensive contributions to the field of chemical synthesis.

Research topics

  • Chemistry
  • Computer Science
  • Organic chemistry
  • Information Retrieval
  • Medicinal chemistry
  • Combinatorial chemistry
  • Computational chemistry
  • Library science
  • World Wide Web
  • Stereochemistry

Selected publications

  • Highly Enantioselective Oxidation Reactions Using a Tetradentate Mn(II) Catalyst Based on ( <i>S</i> , <i>S</i> )-1,2-Diaminocyclohexane

    Organic Letters · 2026-04-08

    articleSenior author

    -1,2-diaminocyclohexane to the highly enantioselective oxidation of a variety of mono-, di-, and trisubstituted olefins or various organosulfur(II) compounds.

  • Highly Position- and Enantioselective Catalytic Epoxidation of Polyolefins Mediated by a Chiral Mn Complex, Including a One-Step Conversion of Squalene to the (<i>S</i>)-2,3-Epoxide, a Precursor of Natural Steroids and Terpenoids

    Journal of the American Chemical Society · 2025-01-06 · 11 citations

    articleSenior authorCorresponding

    Reported herein is the synthesis of a novel chiral dicarboxylic ligand for Mn(II) and the application of the Mn complex to the highly enantio- and position-selective epoxidation of C═C under mild conditions, even with polyolefinic substrates. A stereomechanistic basis for asymmetric induction is suggested.

  • Specific and Strong Acceleration of Nitrosation by Nitrosyl Sulfonates Using the Bis-Coordinating Lewis Acid TiCl<sub>4</sub> or SnCl<sub>4</sub>

    Organic Letters · 2024-01-09 · 3 citations

    articleSenior authorCorresponding

    Nitrosyl triflate is an excellent donor of NO+ to C═C and very unreactive benzenoids, in contrast to the much less reactive nitrosyl mesylate. However, both of these reagents are strongly activated by the bis-coordinating Lewis acids TiCl4 and SnCl4 and become super reactive NO+ donors. Strong catalysis and activation are even observed with the inherently less electrophilic nitrosyl trifluoroacetate. Monocoordinating strong Lewis acids, e.g., MeAlCl2, are relatively ineffective.

  • KIT/PDGFR/Multikinase Inhibitors

    2023-09-08

    otherOpen access1st authorCorresponding

    Activating mutations in platelet-derived growth factor receptor A (PDGFRA) and KIT (a tyrosine kinase encoded by the proto-oncogene c-KIT) account for 82–87% of gastrointestinal stromal tumors (GISTs), the most common type of mesenchymal tumors of the digestive tract. Imatinib, the first multikinase inhibitor that cross-inhibits KIT/PDGFR, was approved by the FDA in 2002 for the treatment of advanced GIST. This chapter describes the discovery process that led to the two FDA-approved second-generation TKIs. Avapritinib is the first precision kinase inhibitor approved in 2020 for adults with unresectable or metastatic GIST harboring a PDGFRA exon 18 mutation, including D842V mutations. Ripretinib was approved in 2020 as a back-up treatment for advanced GIST which is independent of the mutational status of KIT or PDFGRA.

  • KRAS Inhibitors

    2023-09-08

    other1st authorCorresponding

    The RAS protein, a non-kinase, binds to and activates several families of downstream target protein kinases including RAF and PI3K, thereby regulating their signaling pathways. This protein, which serves as a key component of the RAS/RAF/MEK/ERK cascade, is the most frequent oncogenic alteration in human cancers, with KRAS mutations being particularly prevalent in some of the deadliest cancers. This chapter describes the decades-long research that led to the three G12C inhibitors: sotorasib, adagrasib, and JDQ443. Adagrasib, an irreversible inhibitor of the RAS GTPase family, was granted accelerated approval on December 12, 2022, for adult patients with KRAS(G12C) mutated locally advanced or metastatic non-small cell lung cancer (NSCLC), as determined by an FDA-approved test. JDQ443 is a RAS GTPase family covalent inhibitor currently in phase II trial in patients with NSCLC harboring the KRASG12C mutation who have received at least one prior systemic therapy.

  • Appendix 2: Kinase/KRAS Inhibitors in Development <sup>1,2</sup>

    2023-09-08 · 1 citations

    otherOpen access1st authorCorresponding
  • BRAF/Multikinase Inhibitors

    2023-09-08

    other1st authorCorresponding

    Melanoma, the deadliest form of skin cancer, affects more than 1 million Americans annually. Fortunately, the treatment of patients with melanoma has been significantly advanced by the development of molecular-targeted therapies. For example, the BRAFV660E mutation is found in more than half of the patients diagnosed with cutaneous melanoma, making V660E a logical target. In 2011–2018, three BRAF kinase inhibitors were approved for use in the treatment of BRAF mutant melanoma, including vemurafenib, dabrafenib, and encorafenib. Dabrafenib and encorafenib, which are more potent and more selective than the first-approved vemurafenib, can treat patients harboring BRAFV600E or BRAFV600K mutations, whereas vemurafenib is limited to the BRAFV600E-driven melanoma. The development of BRAF-targeted therapies has revolutionized the treatment for BRAF-mutant metastatic melanoma. This chapter describes the discovery process that led to BRAF inhibitors.

  • Appendix 1: First FDA Approvals by Year

    2023-09-08

    otherOpen access1st authorCorresponding
  • PI3K Inhibitors

    2023-09-08

    otherOpen access1st authorCorresponding

    The phosphatidylinositol 3-kinase (PI3K) signaling pathway is frequently aberrantly activated in a variety of cancer types, thus reducing apoptosis and promoting tumor proliferation. This chapter describes the discovery process that led to the five FDA-approved PI3K inhibitors. In 2014, the PI3Kδ inhibitor idelalisib became the first PI3K inhibitor approved for use in specific B cell malignancies. Three year later, the pan-class I PI3K inhibitor copanlisib and the dual PI3Kδ/PI3Kγ inhibitor duvelisib were approved for the same indications. Umbralisib, a dual inhibitor of PI3Kδ and casein kinase-1ε (CK1ε), was approved in 2021 to treat two types of blood cancer: relapsed or refractory marginal zone lymphoma. In 2019, the PI3Kα isoform-selective inhibitor alpelisib was approved for the treatment of advanced breast cancer, in combination with the estrogen receptor downregulator fulvestrant.

  • Other Kinase Inhibitors

    2023-09-08

    otherOpen access1st authorCorresponding

    This chapter describes the research that led to the four FDA-approved kinase inhibitors: netarsudil, belumosudil, fostamatinib, and pexidartinib. Netarsudil is the first trabecular outflow drug approved in 2017 for lowering elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Belumosudil is an orally active Rho kinase 2 inhibitor approved in 2021 for adult and pediatric patients over 12 years of age with chronic graft-versus-host disease after failure of at least two prior lines of systemic therapy. Fostamatinib is the first-in-class spleen tyrosine kinase inhibitor approved by the FDA for the treatment of adults with chronic immune thrombocytopenia who had an insufficient response to previous treatment. Pexidartinib is the first systemic therapy approved in 2019 for adult patients with symptomatic tenosynovial giant cell tumor associated with severe morbidity or functional limitations and not amenable to improvement with surgery.

Frequent coauthors

  • Mark C. Noe

    Pfizer (United States)

    42 shared
  • Robert A. Lewis

    37 shared
  • Do Hyun Ryu

    29 shared
  • Sepehr Sarshar

    26 shared
  • K. Frank Austen

    Harvard University

    21 shared
  • K. Frank Austen

    21 shared
  • C.R. Pace-Asciak

    University of Toronto

    19 shared
  • Michael J. Grogan

    Eli Lilly (United States)

    18 shared

Education

  • B.S., Chemistry

    University of California, Berkeley

    1954
  • Ph.D., Organic Chemistry

    Harvard University

    1959

Awards & honors

  • 1990 Nobel Laureate in Chemistry
  • U.S. National Medal of Science
  • Japan Prize in Science
  • Priestley Medal of the American Chemical Society
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