Letters in organic chemistry

Synthesis and evaluation of an O-Aminated naphthol AS-E as a prodrug of CREB-mediated gene transcription inhibition

F Xie, BX Li, X Xiao

Index: Xie, Fuchun; Li, Bingbing X.; Xiao, Xiangshu Letters in Organic Chemistry, 2013 , vol. 10, # 5 p. 380 - 384

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Citation Number: 2

Abstract

An O-aminated naphthol AS-E was designed as a prodrug to achieve reductive activation and improved aqueous solubility. During the synthesis of this designed compound, a novel transformation from aryl triflates and ethyl acetohydroximate to oxazoles was discovered. Although the initially designed O-amino naphthol AS-E was not made successfully, the eventually synthesized O-tert-butylamino derivative was found to be biologically inactive, ...