Fluorinated Cycloalkyl Building Blocks for Drug Discovery

Area of Science:

• Medicinal Chemistry
• Organic Synthesis
• Drug Discovery

Background:

• Fluorinated cycloalkyl motifs are increasingly important in medicinal chemistry.
• Understanding their synthesis and properties is key to drug design.

Purpose of the Study:

• To review synthetic methods for fluorinated cycloalkyl building blocks.
• To survey their physicochemical properties and biological applications.
• To highlight their role in drug discovery and development.

Main Methods:

• Classical nucleophilic fluorinations.
• Addition of fluorine and heteroatoms to double bonds.
• Cycloadditions and transformations of fluorinated substrates.
• Modern C-H fluorination, decarboxylative, and deborylative fluorinations.

Main Results:

• Fluorinated cycloalkyl groups significantly modulate in vitro parameters like lipophilicity and conformation.
• Various synthetic routes enable access to diverse fluorinated cycloalkyl structures.
• These building blocks are integral to the design of effective therapeutics.

Conclusions:

• Fluorinated cycloalkyl building blocks are versatile tools in modern drug discovery.
• Their strategic incorporation enhances drug properties and efficacy.
• Examples include marketed drugs like Maraviroc, Ivosidenib, and Sitafloxacin.