Expanding the chemical space in practice: diversity-oriented synthesis

Area of Science:

• Organic Chemistry
• Medicinal Chemistry
• Synthetic Chemistry

Background:

• Diversity-Oriented Synthesis (DOS) is crucial for generating novel molecular entities.
• Expanding the accessible chemical space is vital for drug discovery and chemical biology.
• Current synthetic methods often lack the diversity required for comprehensive screening.

Purpose of the Study:

• To dissect the core principles of Diversity-Oriented Synthesis.
• To analyze DOS through the lenses of building block, stereochemical, and skeletal diversity.
• To highlight recent advancements and efficient strategies in DOS.

Main Methods:

• Literature review of recent synthetic methodologies in Diversity-Oriented Synthesis.
• Categorization of DOS strategies based on the type of diversity generated.
• Analysis of key examples demonstrating efficient molecular diversification.

Main Results:

• DOS effectively enhances molecular diversity through strategic combinations.
• Building block, stereochemical, and skeletal diversity are key pillars of DOS.
• Recent literature provides numerous examples of efficient DOS approaches.

Conclusions:

• Diversity-Oriented Synthesis is a powerful paradigm for accessing complex molecular collections.
• The strategic integration of building block, stereochemical, and skeletal diversity is essential for maximizing molecular novelty.
• Continued innovation in DOS will significantly impact drug discovery and materials science.