Benzodiazepines are privileged molecular scaffolds in the field of medicinal chemistry. These molecules are important, as they are abundant among blockbuster drugs and natural products. Thus, there is a continuous demand for the development of more efficient and systematic methods to access such complex molecules. These efforts have found that vinyl-phenyldiaziridines undergo diaza-Claisen rearrangements under thermal conditions to provide the respective benzodiazepines in high yields and diastereoselectivities. This study would provide efficient and continuous access to complex highly functionalized benzodiazepines from simple scaffolds, which will facilitate the engineering of convergent approaches towards more complex heterocyclic pharmacophores.<br/>

Diaza-Claisen rearrangements of substituted diaziridines for the synthesis of benzodiazepines

256th National Meeting (2018)

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