Heck Macrocyclization in Forging Non-Natural Large Rings including Macrocyclic Drugs.

Area of Science:

• Organic Chemistry
• Medicinal Chemistry
• Synthetic Chemistry

Background:

• The intramolecular Heck reaction, or Heck macrocyclization, is a key strategy in natural product total synthesis.
• Its application extends to creating diverse naturally occurring macrocycles.
• However, its utility in synthesizing non-natural macrocycles is less explored.

Purpose of the Study:

• To systematically review the application of Heck macrocyclization in forging non-natural macrocycles.
• To highlight the significance of this reaction in areas beyond natural product synthesis.
• To focus on the role of Heck macrocyclization in drug discovery and synthetic methodology development.

Main Methods:

• Literature review focusing on Heck macrocyclization for non-natural macrocycle synthesis.
• Categorization of applications into drug discovery research and synthetic methodology development.
• Analysis of case studies demonstrating the formation of synthetic macrocycles.

Main Results:

• Heck macrocyclization is a powerful tool for creating novel synthetic macrocycles of non-natural origin.
• The reaction plays a remarkable role in drug discovery research, leading to potential therapeutic agents.
• It also contributes significantly to the development of new synthetic methodologies for complex molecules.

Conclusions:

• Heck macrocyclization is a versatile strategy with broad applications in synthetic chemistry.
• Its impact on generating non-natural macrocycles, especially in medicinal chemistry, is substantial.
• This review underscores the underappreciated value of Heck macrocyclization in creating synthetic macrocycles, including macrocyclic drugs.