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Alkyl Sulfinates: Radical Precursors Enabling Drug Discovery.

Joel M Smith1, Janice A Dixon1, Justine N deGruyter1

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Sulfinates, now called Diversinates, are rapidly adopted in drug discovery for reaction validation. This review highlights over 50 compelling recent examples to identify predictable reactivity trends.

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Area of Science:

  • Medicinal Chemistry
  • Organic Synthesis
  • Drug Discovery

Background:

  • Modern drug discovery necessitates rigorous validation of new chemical reactions.
  • Sulfinates, marketed as Diversinates, have gained significant traction in medicinal chemistry.
  • Numerous patents and primary reports demonstrate their increasing use.

Purpose of the Study:

  • To review compelling applications of sulfinates in medicinal chemistry over the past five years.
  • To identify robust and predictable trends in sulfinate reactivity.
  • To aid in the validation process for new drug discovery reactions.

Main Methods:

  • Comprehensive literature search of primary reports and patents.
  • Analysis of over 50 published examples of sulfinate reactions.
  • Identification and categorization of reactivity patterns and trends.

Main Results:

  • Demonstrated alacritous adoption of sulfinates by the medicinal chemistry community.
  • Highlighted over 50 compelling use cases from the last five years.
  • Identified key trends in sulfinate reactivity, supporting their predictability.

Conclusions:

  • Sulfinates (Diversinates) are a validated and increasingly utilized tool in drug discovery.
  • The reviewed examples provide a foundation for understanding and predicting sulfinate reactivity.
  • This work supports the rigorous validation required for implementing new reactions in drug development.