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Org Biomol Chem 2025, in press

DOI: 10.1039/d4ob01669f

Iermolenko I.; Artemenko A.; Vasko D.; Shcherbyna A.; Datsenko O.; Ostapchuk E. et al.

This article describes concise and practical synthetic approaches toward the multigram-scale preparation of value-added conformationally constrained 5-spirocyclic α-prolines from readily accessible starting materials. Direct carboxylation of 2-spiropyrrolidines is a novel and promising approach to achieve this goal, particularly for substrates with no acidic centers within the spiro-linked portion of the pyrrolidine core. The method allows for quick, one-step preparation of the target chemicals in good yields. An alternative synthetic avenue was designed for substrates unsuitable for direct carboxylation. This 4-step protocol involves common laboratory practice transformations and is comparable in its efficiency to the carboxylation method. This study concludes a series of our investigations on the elaboration of efficient methods for the construction of spiro-proline frameworks.

 

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