According to an informal survey of our drug discovery colleagues outside the synthetic community, our syntheses typically consist of six steps, predominantly composed of amine deprotections to facilitate amide formation reactions and Suzuki couplings to produce biaryl derivatives, resulting in large, flat, achiral derivatives destined for screening cascades.To investigate these pre-conceptions, we have analysed a subset of medicinal chemistry programmes to determine what comprises the �Medicinal Chemist's toolbox�, and whether these pre-conceptions are truly representative of the medicinal chemist's output. This analysis includes the synthesis of more than 3500 final, screened compounds described in 150 high-impact publications. The analysis reveals some interesting trends, highlights troubling consequences and suggests potential areas for further synthetic development. Importantly, our analysis suggests that to break from the rigid physical property (and possibly off-target toxicity) liabilities these properties often entail, there is a need to employ alternate methodology to prepare more varied compounds.

What do (medicinal) chemists do all day? (And what does it mean for our molecules?)

243rd National Meeting (2012)

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