Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production
摘要:
A series of diphenyl ethers was prepared and evaluated for androgen receptor antagonist activity in human androgen receptor binding and cellular functional assays. Analogs with potent in vitro activities were evaluated for topical in vivo efficacy in the Golden Syrian Hamster ear model. Several compounds showed reduction in wax esters in this validated animal model. (C) 2009 Elsevier Ltd. All rights reserved.
Copper-catalyzed <i>O</i>-arylation of phenols with diazonium salts
作者:Xin Fang、Chengning Qi、Xiangqian Cao、Zhi-Gang Ren、David James Young、Hong-Xi Li
DOI:10.1039/d3gc02541a
日期:——
It is well known that diazonium salts (ArN2+) react with phenols (Ar′OH) to give aryl diazoethers or diazo compounds, but their cross-coupling to exclusively access diaryl ethers is challenging. Herein we disclose the Cu-catalyzed etherification of phenols with aryl diazonium salts at room temperature, yielding diaryl ethers in moderate to excellent yields. The advantages of this protocol are mild