Target Oriented Organic Synthesis and Retrosynthetic Analysis, Focussed Libraries, Bicylic Ketone, Diels-Alder Reaction

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Target-oriented Organic Synthesis and Retrosynthetic Analysis

Target-oriented synthesis has benefitted from a powerful planning algorithm, the retrosynthetic analysis, which involves recognition of the key structural elements in the product to be synthesized. In this approach, which became available in 1990s, the chemist starts with a structurally complex compound and finds simpler compounds (also called 'building blocks') that can be used to start the synthesis of the putative drug.

For the chemist, this drug compound to be synthesized (not the cellular protein that needs to be reached by the drug), is called the target, hence the term target-oriented synthesis. "Focussed libraries" of target compounds (possible future drugs) are also used for retrosynthetic analysis. Since in this approach, we move in the reverse direction of the reaction (product to substrate) to identify the substrates to be used for synthesis, we call it retrosynthetic analysis.

The retrosynthetic analysis is actually sine qua non (essential requirement) of the target-oriented synthesis in drug discovery. An example of retrosynthetic analsis to plan a target-oriented synthesis is shown. In this figure, the target for synthesis is a cis-fused bicyclic ring containing olefin and ketone functionalities. Retrosynthetic analysis suggests that bridged bicyclic ketone is the product of a Diels-Alder reaction, in which simple starting materials, cyclohexadiene and ketene are used as reactants.

Similarly, the above cis-fused bicyclic ring containing olefin and ketone is also the product of a oxy-Cope rearrangement reaction, if we start with vinyl and hydroxyl groups attached to a ring carbon. The readers are advised to consult a chemistry book for Diels-Alder and oxy-Cope reactions that are used widely for target-oriented synthesis for drug discovery

Principle of restrosynthetic analysis and its use to plan target oriented for development of two anticancer drugs

Principle involved in retrosynthetic analysis

An example of retrosynthetic analysis

An example of retrosynthetic analysis

Two anticancer molecules synthesized using retrosynthetic analysis

Two anticancer molecules synthesized using retrosynthetic analysis

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