[EN] 1,4-DISUBSTITUTED PIPERIDINE DERIVATIVES AND THEIR USE AS 11-BETAHSD1 INHIBITORS<br/>[FR] DERIVES DE PIPERIDINE 1,4 DISUBSTITUEE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE 11-BETAHSD1
申请人:ASTRAZENECA AB
公开号:WO2004033427A1
公开(公告)日:2004-04-22
The use of a compound of formula (I) in the manufacture of a medicament for use in the inhibition of 11βHSD1 is described.
使用式(I)的化合物制造用于抑制11βHSD1的药物。
An Efficient and General Method for the Heck and Buchwald–Hartwig Coupling Reactions of Aryl Chlorides
作者:Dong-Hwan Lee、Abu Taher、Shahin Hossain、Myung-Jong Jin
DOI:10.1021/ol202177k
日期:2011.10.21
The β-diketiminatophosphane Pd complex acted as a powerful catalyst for the Heck coupling of aryl chlorides with alkenes. Various aryl and heteroaryl chlorides were coupled efficiently under relatively mild conditions. Furthermore, this catalytic system also proved to be highly active in the Buchwald–Hartwig coupling of deactivated and sterically hindered aryl chlorides at room temperature.
α-Ketoacids can be easily synthesized with satisfactory yields and selectivities by carbonylation of aryl halides and secondary benzyl halides under very mild conditions. The reactions are catalyzed by Co2(CO)8 in alcoholic solvents; the presence of a methyl source (dimethyl sulfate or methyl iodide) is necessary for the carbonylation of the aryl halides. Base, temperature and solvent have large effects on the
Aqueous Copper Nitrate Catalyzed Synthesis of 3-Alkylideneoxindoles from α-Diazo-β-ketoanilides
作者:Shanyan Mo、Zhanhui Yang、Jiaxi Xu
DOI:10.1002/ejoc.201402206
日期:2014.6
An economical, practical, and green protocol with which to synthesize 3-alkylideneoxindolesfromα-diazo-β-ketoanilides has been developed. The approach employs inexpensive Cu(NO3)2·3H2O as catalyst and environmentally friendly water as solvent, and achieves moderate to excellent yields. The method has good tolerance to a range of N-alkyl and N-aryl groups, including electron-withdrawing and electron-donating
Substituted homopiperidine, piperidine or pyrrolidine derivatives
申请人:Sorensen Lindy Jan
公开号:US20050107434A1
公开(公告)日:2005-05-19
A novel class of substituted homopiperidine, piperidine and pyrrolidine derivatives, methods for their preparation, pharmaceutical compositions comprising them and use thereof in the treatment of disorders related to the histamine H3 receptor. More particularly, the compounds possess histamine H3 receptor antagonistic activity and are thus useful in the treatment of disorders in which a histamine H3 receptor blockade is beneficial.