Direct ortho-C–H Functionalization of Aromatic Alcohols Masked by Acetone Oxime Ether via exo-Palladacycle
摘要:
Use of an iridium catalyst allowed the efficient dehydrogenative functionalization of C-H bonds of azulenes with the production of hydrogen as the sole byproduct. The reaction occurred with excellent chemo- and regioselectivities to provide 2-silylazulenes even without any directing groups. Effective conjugation through the 2-position of the azulene ring was demonstrated by the unique stimuli-responsiveness against an acidbase reaction.
HETEROCYCLIC MODULATORS OF HIF ACTIVITY FOR TREATMENT OF DISEASE
申请人:Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer Center
公开号:US20140073634A1
公开(公告)日:2014-03-13
The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.
Direct <i>ortho</i>-C–H Functionalization of Aromatic Alcohols Masked by Acetone Oxime Ether via <i>exo</i>-Palladacycle
Use of an iridium catalyst allowed the efficient dehydrogenative functionalization of C-H bonds of azulenes with the production of hydrogen as the sole byproduct. The reaction occurred with excellent chemo- and regioselectivities to provide 2-silylazulenes even without any directing groups. Effective conjugation through the 2-position of the azulene ring was demonstrated by the unique stimuli-responsiveness against an acidbase reaction.
Palladium-catalyzed direct <i>mono</i>-aroylation of <i>O</i>-arylmethyl and aryl-substituted acetoxime ethers
作者:Ling-Yan Shao、Zhi Xu、Cun-Ying Wang、Xiao-Pan Fu、Miao-Miao Chen、Hong-Wei Liu、Ya-Fei Ji
DOI:10.1039/c8ob01400k
日期:——
An efficient palladium-catalyzed ortho-aroylation of O-arylmethyl and aryl-substituted acetoxime ethers has been developed; this method has high mono-site selectivity and does not require exogenous ligands. Under the direction of a simple exo-acetoxime auxiliary, a broad scope of masked arylmethyl alcohols and phenols as well as various aromatic aldehydes are compatible with this transformation, which
已经开发出一种有效的钯催化的O-芳基甲基和芳基取代的乙肟醚的邻芳基化反应。这种方法具有较高的单上门的选择性,并且不需要外源性配体。在简单的外切-乙酰肟辅助剂的指导下,各种掩蔽的芳基甲醇和苯酚以及各种芳族醛均与这种转化相容,这很可能遵循一种涉及六元或五元外-环palpalated中间体的机制途径。可以方便地采用该策略来制备具有合成价值的1 H-苯并[ d ] [1,2]恶嗪和苯并[ d]异恶唑。可以容易地从产物中除去导向基团,以提供官能化的二芳基酮。