[Diversity-oriented synthesis and its application in drug discovery]

Area of Science:

• Medicinal Chemistry
• Organic Synthesis

Background:

• Diversity-oriented synthesis (DOS) is crucial for generating molecular collections with varied structures.
• Diverse molecular scaffolds are essential for exploring biological processes and identifying drug candidates.

Purpose of the Study:

• To review common strategies in diversity-oriented synthesis.
• To highlight recent literature examples of DOS applications.
• To present the use of DOS libraries in drug discovery.

Main Methods:

• Discussion of reagent-based and substrate-based approaches.
• Explanation of the build-couple-pair strategy.
• Overview of privileged substructure-based DOS.

Main Results:

• Common DOS strategies are detailed with literature examples.
• The review covers diverse molecular features like appendages, functional groups, stereochemistry, and skeletons.
• Applications of DOS libraries in drug discovery are presented.

Conclusions:

• Diversity-oriented synthesis provides a powerful platform for generating molecular diversity.
• The reviewed strategies enable the creation of compound libraries for biological screening.
• DOS plays a significant role in advancing drug discovery efforts.