Diversity-oriented synthesis (DOS) aims at the efficient synthesis of structurally diverse compound collections. Macrocycles represent an underexplored structural class in drug discovery although having shown high affinity and selectivity for protein targets as well as suitable pharmacokinetic properties.Here we report the diversity-oriented synthesis of a diverse collection of novel macrocyclic scaffolds comprising heterocyclic moieties such as hydantoins, dihydrouracils, oxalylureas, and triazoles. These compounds were prepared from a common precursor in not more than three steps.

Diversity-oriented synthesis of macrocyclic scaffolds

243rd National Meeting (2012)

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