Diethylaminosulfur trifluoride-mediated intramolecular cyclization of 2-hydroxycycloalkylureas to fused bicyclic aminooxazoline compounds and evaluation of their …

…, W Wang, D Smith, G Vigers, D Dutcher, KW Hunt…

Index: Huestis, Malcolm P.; Liu, Wendy; Volgraf, Matthew; Purkey, Hans E.; Yu, Christine; Wang, Weiru; Smith, Darin; Vigers, Guy; Dutcher, Darrin; Hunt, Kevin W.; Siu, Michael Tetrahedron Letters, 2013 , vol. 54, # 43 p. 5802 - 5807

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Citation Number: 3

Abstract

Abstract A series of unique bicyclic aminooxazolines were synthesized and found to exhibit micromolar inhibition of β-secretase-1 (BACE-1). The aminooxazolines were procured by an intramolecular diethylaminosulfur trifluoride (DAST)-mediated ring closure of a benzylic urea onto a secondary alcohol.