Synthesis of 4-Substituted Chlorophthalazines, Dihydrobenzoazepinediones, 2-Pyrazolylbenzoic Acid, and 2-Pyrazolylbenzohydrazide via 3-Substituted 3-Hydroxyisoindolin-1-ones
作者:Hanh Nho Nguyen、Victor J. Cee、Holly L. Deak、Bingfan Du、Kathleen Panter Faber、Hakan Gunaydin、Brian L. Hodous、Steven L. Hollis、Paul H. Krolikowski、Philip R. Olivieri、Vinod F. Patel、Karina Romero、Laurie B. Schenkel、Stephanie D. Geuns-Meyer
DOI:10.1021/jo3000628
日期:2012.4.20
hydrazine, followed by chlorination with POCl3. We have also discovered twonovel transformations of 3-vinyl- and 3-alkynyl-3-hydroxyisoindolinones. Addition of vinyl organometallic reagents to N,N-dimethylaminophthalimide (8a) provided dihydrobenzoazepinediones 15a–15c via the proposed ringexpansion of 3-vinyl-3-hydroxyisoindolinone intermediates. 3-Alkynyl-3-hydroxyisoindolinones react with hydrazine and
[structure: see text] The totalsynthesis of (-)-21-isopentenylpaxilline (1) has been achieved. Key elements of the synthesis include the stereocontrolledconstruction of the advanced eastern hemisphere (-)-5, a highly efficient union of the eastern and western fragments (-)-5 and 4, respectively, exploiting our 2-substituted indole synthesis, and a new protocol for the construction of ring C.
Copper-Catalyzed Amino Lactonization and Amino Oxygenation of Alkenes Using <i>O</i>-Benzoylhydroxylamines
作者:Brett N. Hemric、Kun Shen、Qiu Wang
DOI:10.1021/jacs.6b02840
日期:2016.5.11
A copper-catalyzed amino lactonization of unsaturated carboxylic acids has been achieved as well as the analogous intermolecular three-component amino oxygenation of olefins. The transformation features mild conditions and a remarkably broad substrate scope, offering a novel and efficient approach to construct a wide range of amino lactones as well as 1,2-amino alcohol derivatives. Mechanistic studies
[EN] AZETIDIN-3-YLMETHANOL DERIVATIVES AS CCR6 RECEPTOR MODULATORS<br/>[FR] DÉRIVÉS D'AZÉTIDIN-3-YLMÉTHANOL EN TANT QUE MODULATEURS DU RÉCEPTEUR CCR6
申请人:IDORSIA PHARMACEUTICALS LTD
公开号:WO2021219849A1
公开(公告)日:2021-11-04
The present invention relates to compounds of Formula (I), their synthesis and use as CCR6 receptor modulators for the treatment or prevention of various diseases, conditions or disorders.
本发明涉及式(I)化合物,其合成以及作为CCR6受体调节剂用于治疗或预防各种疾病、状况或障碍。
Anomalous Staudinger reaction at intramolecular frustrated P–B Lewis pair frameworks
作者:Annika Stute、Lukas Heletta、Roland Fröhlich、Constantin G. Daniliuc、Gerald Kehr、Gerhard Erker
DOI:10.1039/c2cc36782c
日期:——
The FLP-mesityl azide addition products 5, formed by FLP-addition to the terminal azide nitrogen atom, undergo N-N bond cleavage in an unusual variant of the Staudinger reaction upon thermolysis or photolysis to give an internally borane stabilized [P]=NH phosphinimine and a dimethylindazole derivative.