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Retrosynthetic Analysis: Planning the Route to Drug Synthesis

Abstract

Weingart Houdeau

The process of drug synthesis is a complex and intricate task that involves the transformation of raw chemical materials into a therapeutic compound with specific biological activities. One of the key strategies employed in the design and synthesis of pharmaceuticals is retrosynthetic analysis. This powerful method, pioneered by Nobel laureate Elias James Corey, allows chemists to deconstruct a target molecule into simpler precursor molecules, ultimately guiding the synthesis backward from the final product to readily available starting materials. Retrosynthetic analysis is an indispensable tool in the field of organic chemistry, providing a systematic approach to planning the most efficient and feasible route for drug synthesis. Retrosynthetic analysis relies on the identification of key functional groups and strategic disconnections within a target molecule. The goal is to simplify the complex structure of the target compound into smaller, more accessible fragments. This process involves breaking down carbon-carbon and carbon-heteroatom bonds in a way that allows for the retrosynthetic intermediates to be easily sourced or synthesized. Chemists often use protective groups and selective reactions to control the regio-chemistry and stereochemistry of the synthetic steps.

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