Conformational restriction is an effective tool used in medicinal chemistry to improve/modify pharmacological profiles of lead compounds. Due to a fixation of the functional groups in a biologically active conformation, the sterically restricted compounds are often more efficient and selective ligands for various targets, thus displaying pronounced biological activity.1 In this work, we synthesized a library of novel conformationally restricted bicyclic scaffolds by Double-Mannich reaction of cyclic ketones. Details of the synthesis and application of the obtained compounds will be discussed. 1 T. Druzhenko et al. 2014 Manuscript under preparation 2 A. Mityuk et al. Synthesis 2010, 493. 3 O. Denisenko et al. Tetrahedron Lett. 2010, 51, 1790. 4 O. Denisenko et al. Org. Lett. 2010, 12, 4372.

Synthesis of conformationally restricted scaffolds by double-Mannich reaction of cyclic ketones

249th National Meeting (2015)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.