4.7 Article

Alkyl Sulfinates: Radical Precursors Enabling Drug Discovery

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 62, Issue 5, Pages 2256-2264

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.8b01303

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Funding

  1. Arnold and Mabel Beckman Foundation
  2. Bristol-Myers Squibb
  3. Pfizer Inc.
  4. LEO Pharma

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The modern constraints of drug discovery demand a rigorous validation process of all new reactions prior to widespread implementation. To this end, sulfinates (now marketed as Diversinates) have seen alacritous adoption by the medicinal chemistry community, as evidenced by the recent outpour of both patent and primary reports. Featuring more than 50 examples, this review seeks to highlight those particularly compelling cases published in the past 5 years, with an eye toward the identification of robust and predictable trends in reactivity.

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