Dioxazolones as masked ester surrogates in the Pd(<scp>ii</scp>)-catalyzed direct C–H arylation of 6,5-fused heterocycles
作者:Paridhi Saxena、Neha Maida、Manmohan Kapur
DOI:10.1039/c9cc05563k
日期:——
simple and effective Pd(II)-catalyzed regioselectiveC(2)–H arylation of 6,5-fused heterocycles with dioxazolones as a masked ester surrogate undermildconditions is reported. The significance of the arylation is highlighted by the new reactivity demonstrated in dioxazolones via proximal C–H activation of the cyclic carbonate of the hydroxamic acid functionalityunder protic conditions.
Copper‐Catalyzed Ring Opening of Benzofurans and an Enantioselective Hydroamination Cascade
作者:Qing‐Feng Xu‐Xu、Qiang‐Qiang Liu、Xiao Zhang、Shu‐Li You
DOI:10.1002/anie.201809003
日期:2018.11.12
A copper(II) acetate/(R)‐DTBM‐SEGPHOS‐catalyzed ring opening of benzofurans and enantioselective hydroamination cascade with dimethoxymethylsilane (DMMS) and hydroxylamine esters is described. Starting from readily available substituted benzofurans, a series of chiral N,N‐dibenzylaminophenols, which are of high interest in pharmaceutical chemistry, were obtained with excellent enantioselectivities (up
Zeolite-catalyzed synthesis of 2,3-unsubstituted benzo[b]furans via the intramolecular cyclization of 2-aryloxyacetaldehyde acetals
作者:Nan Sun、Peng Huang、Yifan Wang、Weimin Mo、Baoxiang Hu、Zhenlu Shen、Xinquan Hu
DOI:10.1016/j.tet.2015.05.029
日期:2015.7
An efficient and environmentally benign heterogeneous catalytic process for the synthesis of 2,3-unsubstituted benzo[b]furans has been established via the intramolecular cyclization of 2-aryloxyacetaldehyde acetals. By utilizing tin-exchanged H-β zeolite (Sn-β) as catalyst, a wide range of functionalized 2,3-unsubstituted benzo[b]furans could be prepared in good to excellent yields. The Sn-β zeolite
通过2-芳氧基乙醛缩醛的分子内环化,已经建立了一种有效的,对环境无害的非均相催化方法,用于合成2,3-未取代的苯并[ b ]呋喃。通过使用锡交换的H-β沸石(Sn-β)作为催化剂,可以以良好或极好的收率制备各种功能化的2,3-未取代的苯并[ b ]呋喃。Sn-β沸石催化剂还在间位取代的2-芳氧基乙醛缩醛的环化上表现出优异的形状选择性,并且优选形成高达97%的区域选择性的6-取代的异构体。而且,Sn-β沸石可以容易地回收和再利用而没有任何明显的活性损失。
Visible light-induced monofluoromethylenation of heteroarenes with ethyl bromofluoroacetate
作者:Wei Yu、Xiu-Hua Xu、Feng-Ling Qing
DOI:10.1039/c6nj00281a
日期:——
A mild approach for the directintroduction of an ethoxycarbonylmonofluoromethyl group into heteroarenesvia visible light photocatalysis has been developed.
The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behcet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.