Abstract

Pyrazolidin-3-ones derivatives, including 5oxopyrazolidine-1-carboximidamides, are an important class of compounds, which possess widespread pharmacological properties such as analgesic, antipyretic and anticancer. Several synthetic approaches have been developed to access pyrazolidin-3-one rings. In this work we disclose a facile and diastereoselective synthetic approach to prepare oxopyrazolidine-1carboximidamides derivatives from Morita-BaylisHillman (MBH) adducts. Our approach is based on a tandem sequence involving a Michael addition reaction and cyclization, which forms in a single step a new cycle and controls the relative stereochemistry of two centers.

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