A number of bioactive molecules possess a 3,3-dimethylazetidine moiety. An iodine-mediated intramolecular cyclization reaction of γ-prenylated amines has been developed to provide a convenient route to 3,3-dimethylazetidines in a highly diastereoselective manner. The presented approach not only offers a new strategy for the synthesis of the bioactively important 3,3-dimethylazetidines but also provides an opportunity to extend the application of γ-prenylated amine synthons in organic synthesis.

This study developed a diastereoselective synthesis strategy for 3,3-dimethylazetidines, offering a new strategy for bioactive molecules and extending the application of -prenylated amine synthons in organic synthesis.

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Diastereoselective synthesis of 3,3-dimethylazetidines via an intramolecular iodine-mediated cyclization reaction

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