Five-membered nitrogen containing heterocycles have been principally important in many natural compounds and successful medicines. We were able to develop a root to the synthesis of novel scaffold based on 5-benzoyl-2-oxo-4-phenylpyrrolidine-3-carbonitrile. The root involves a 3-step synthesis, including a final step of conversion of intermediate highly substituted 2-aminopyrrolines into 2-oxopyrrolidines using formic acid, which to the best of our knowledge was performed for the first time. A small library of new compounds was synthesized and characterized. Their biological activity was evaluated against B16 mice melanoma cells using MTT assay. It was found that the majority of compounds possess low micro molar, or even sub-micro molar, cytotoxicity.

Multi-step synthesis and evaluation of cytotoxicity in diversely functional 2-oxopyrrolidines

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