4.4 Article

Diastereoselective scalable synthesis of 2,6-trans-Piperidines using an aza-Michael reaction

Journal

TETRAHEDRON LETTERS
Volume 60, Issue 4, Pages 371-374

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2018.12.061

Keywords

trans-piperidine; aza-Michael cyclization; Diastereoselective; Base catalyzed; tert-butanesulfinamide

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Highly efficient substrate and reagent controlled stereoselective synthesis of 2,6-trans-piperidine derivative (1) using an aza-Michael reaction is reported. This method was utilized to synthesize a variety of trans-piperidines on hundred-gram scales. (C) 2018 Elsevier Ltd. All rights reserved.

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