Highly efficient asymmetric construction of novel indolines and tetrahydroquinoline derivatives <i>via</i> aza-Barbier/C–N coupling reaction
作者:Tao Guo、Bin-Hua Yuan、Wen-Jie Liu
DOI:10.1039/c7ob02891a
日期:——
Highly stereoselectivesyntheses of chiral indolines and tetrahydroquinolines are achieved by combining the asymmetric Zn-mediated allylation of chiral N-tert-butanesulfinyl imines with efficient intramolecular C–N cross-coupling. Herein, the advantages of such a synthetic strategy are illustrated by the synthesis of indolines and tetrahydroquinolines with quaternary stereocenters and multi-substituted
Herein, we report a new process for the synthesis of highlyfunctionalizedpyridines based on a tandem Pummerer-type rearrangement, aza-Prins cyclization, and elimination-induced aromatization. This formal [5+1] cyclization provides pyridines in good yields with easily accessible starting materials. The synthetic potential of our new method is further demonstrated in the modification of the frameworks
Thermolysis-Induced Two- or Multicomponent Tandem Reactions Involving Isocyanides and Sulfenic-Acid-Generating Sulfoxides: Access to Diverse Sulfur-Containing Functional Scaffolds
作者:Shengfeng Wu、Xiaofang Lei、Erkang Fan、Zhihua Sun
DOI:10.1021/acs.orglett.7b03593
日期:2018.2.2
Direct reaction of isocyanides with some sulfenic-acid-generating sulfoxides led to the effective formation of the corresponding thiocarbamic acid S-esters in good to high yields. A multicomponent reaction involving isocyanide, sulfoxide, and a suitable nucleophile has also been developed, providing ready access to a diverse range of sulfur-containing compounds, including isothioureas, carbonimidothioic
[EN] PYRROLO [2, 3 - B] PYRAZINE - 7 - CARBOXAMIDE DERIVATIVES AND THEIR USE AS JAK AND SYK INHIBITORS<br/>[FR] DÉRIVÉS DE PYRROLO[2,3-B]PYRAZINE-7-CARBOXAMIDE ET LEUR UTILISATION COMME INHIBITEURS DE JAK ET SYK
申请人:HOFFMANN LA ROCHE
公开号:WO2011144585A1
公开(公告)日:2011-11-24
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula (I), wherein the variables Q and R, R2, and R3 are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
Acid-Catalyzed Synthesis of Aryl[4,5]isothiazoles through a Sulfenic Acid Pathway
作者:Hong Yuan、Zhihua Sun
DOI:10.1055/s-0039-1690201
日期:2019.10
A new method to efficiently prepare 3-substituted aryl[4,5]isothiazoles by simply heating the starting materials with a catalytic amount of p-toluenesulfonic acid in toluene is reported. This simple procedure is well suitable for a variety of substrates that can tolerate substitution changes in the fusing aromatic ring, as well as at the 3-position. Substituted aryl rings of varying electronic properties