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Late-Stage Fluorination: From Fundamentals to Application.

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This review covers late-stage fluorination methods for small molecules, emphasizing practical industrial applications. We critically assess current developments for their real-world utility and potential.

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Area of Science:

  • Organic Chemistry
  • Medicinal Chemistry
  • Chemical Synthesis

Background:

  • Late-stage functionalization is crucial for drug discovery and development.
  • Introducing fluorine and fluorinated groups can significantly alter molecular properties.
  • Efficient methods for late-stage fluorination are highly sought after in the pharmaceutical industry.

Approach:

  • This work reviews laboratory findings on late-stage introduction of fluorine.
  • Focuses on practical developments with potential industrial applications.
  • Critically evaluates methods for their current utility and future prospects.

Key Points:

  • Highlights successful late-stage fluorination strategies.
  • Discusses the incorporation of fluorinated functional groups into small molecules.
  • Assesses the scalability and applicability of reviewed methods for industrial use.

Conclusions:

  • Several practical developments in late-stage fluorination show promise for industrial applications.
  • Further critical evaluation is needed for methods not yet meeting practical use standards.
  • This review provides insights into advancing fluorination chemistry for small molecule synthesis.