Synthetic methods for oxidative aromatic C-O bond formation are sparse, despite their demand in metabolite synthesis for drug discovery and development. We report a novel methodology for late-stage C-O bond formation of arenes. The reaction proceeds with excellent functional group tolerance even for highly functionalized substrates. The resulting aryl mesylates provide access to potential human metabolites
尽管在药物发现和开发中需要代谢物合成,但用于形成氧化芳族 CO 键的合成方法很少。我们报告了一种用于芳烃后期 CO 键形成的新方法。即使对于高度官能化的底物,该反应也以优异的官能团耐受性进行。所得的甲磺酸芳基酯提供了获取潜在的人类药物代谢物的途径,并可直接用于安装 CF 键以阻断代谢热点。试剂双(甲磺酰基)过氧化物和底物芳烃之间的电荷转移相互作用可能与芳烃相对于其他官能团的化学选择性官能化有关。
PIPERAZINE COMPOUNDS WITH A HERBICIDAL ACTION
申请人:Hupe Eike
公开号:US20090156553A1
公开(公告)日:2009-06-18
The invention relates to the use of piperazine compounds of formula (I) or the agriculturally useful salts of piperazine compounds of formula (I) as herbicides, the variables in formula (I) being defined as cited in the claims and the description.
The invention is concerned with a UV absorbing plastics material to be used in intraocular lenses, said material having been produced by means of incorporating in the plastics monomer mixture, prior to the polymerization thereof, a combination of chromophores selected from two groups of substances.
Chromatography-Free and Eco-Friendly Synthesis of Aryl Tosylates and Mesylates
作者:Xiangyang Lei、Anusha Jalla、Mhd Abou Shama、Jamie Stafford、Billy Cao
DOI:10.1055/s-0034-1378867
日期:——
Two chromatography-free and eco-friendly protocols have been developed to synthesize aryl tosylates and mesylates by the tosylation and mesylation of the corresponding hydroxyarenes, respectively. These protocols are superior to other known ones regarding the simplicity, reaction time and conditions, the range of substrates, yields, and environmental friendliness.