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γ-Aminoalcohol rearrangement applied to pentahydroxylated azepanes provides pyrrolidines epimeric to homoDMDP†
Y. Jagadeesh,A. T. Tran,B. Luo,N. Auberger,J. Désiré,S. Nakagawa,A. Kato,Y. Zhang,M. Sollogoub,Y. Blériot
Organic & Biomolecular Chemistry Pub Date : 01/29/2015 00:00:00 , DOI:10.1039/C5OB00050E
Abstract

A series of pentahydroxylated pyrrolidines, displaying five contiguous stereogenic centres and epimeric to α-glucosidase inhibitor homoDMDP, have been synthesized. The key step involves a γ-aminoalcohol rearrangement applied to polyhydroxylated azepanes. These five-membered iminosugars demonstrate micromolar inhibition of glycosidases.

Graphical abstract: γ-Aminoalcohol rearrangement applied to pentahydroxylated azepanes provides pyrrolidines epimeric to homoDMDP
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