Three-membered ring nitrogen-containing heterocycles are privileged pharmacophores in the field of medicinal chemistry. These heterocyclic molecules are key chemical building blocks for the synthesis of several blockbuster drugs and natural products. Thus, there is a continuous demand for the development of more efficient and systematic methods to access them. We have found that substituted isocyanates and chloramines under acidic conditions provide the corresponding asymmetrical diaziridinones in good yields. This study would provide efficient and continuous access to complex highly functionalized heterocycles from simple scaffolds, which will facilitate the engineering of convergent approaches towards more complex heterocyclic pharmacophores.

Novel synthesis of asymmetrical substituted diaziridinones from simple isocyanates

254th National Meeting (2017)

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