Recyclable [bmIm]OH promoted one-pot heterocyclization: synthesis of substituted benzofurans
摘要:
A single step access to polysubstituted benzo[b]furans has been achieved under simple and eco-compatible conditions. The heterocyclization proceeded efficiently. [bmIm]OH played a triple role as a solvent, base as well as catalyst. (C) 2013 Elsevier Ltd. All rights reserved.
Sequential and One-Pot Reactions of Phenols with Bromoalkynes for the Synthesis of (<i>Z</i>)-2-Bromovinyl Phenyl Ethers and Benzo[<i>b</i>]furans
作者:Shihua Wang、Pinhua Li、Lin Yu、Lei Wang
DOI:10.1021/ol202383z
日期:2011.11.18
2-substituted benzo[b]furans in good yields throughpalladium-catalyzeddirect C–H bond functionalizations. It is important to note that the transformation of phenols with bromoalkynes into benzo[b]furans could be carried out in one pot with a simple and efficient tandem procedure.
苯并[ b ]呋喃在一个锅中根据苯酚与溴炔烃的加成/钯催化的CH键结合官能化制备。苯酚与溴代炔烃的加成反应以高收率生成了具有优异区域和立体选择性的(Z)-2-溴乙烯基苯基醚。所获得的(Z)-2-溴乙烯基苯基醚随后通过分子内环化进行处理,通过钯催化的直接C–H键官能化,以高收率获得了2-取代的苯并[ b ]呋喃。重要的是要注意,可以将溴代炔烃将苯酚转化为苯并[ b ]呋喃,可以通过简单而有效的串联程序在一个罐中进行。
A Highly Efficient Tandem Reaction of 2-(gem-Dibromovinyl)phenols(thiophenols) with Organosilanes to 2-Arylbenzofurans (thiophenes)
作者:Jie Liu、Wei Chen、Yong Ji、Lei Wang
DOI:10.1002/adsc.201100875
日期:2012.5.21
cross‐coupling reaction. In the presence of tetra‐(n‐butyl)ammonium fluoride (TBAF), palladium(II) acetate [Pd(OAc)2] and triphenylphosphine (PPh3), the reaction of 2‐(gem‐dibromovinyl)phenols(thiophenols) with phenyl(trialkoxy)silanes proceeded smoothly and generated the corresponding products with good yields in one‐pot. It should be noted that TBAF plays an important role in the tandem reaction.
The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT
2
) receptor. More particularly the invention relates to piperidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT
2
receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.