在温和且可扩展的电解条件下,已开发出无金属和无氧化剂的分子内脱氢N–N键的形成。从容易获得的N-(2-吡啶基)am有效地合成了各种有价值的1,2,4-三唑并[1,5- a ]吡啶。反应在恒定电流条件下,在简单的不分隔电池中进行,其中n Bu 4 NBr作为氧化还原介体和电解质。该方案适用于抗糖尿病化合物关键中间体的有效合成。
[EN] HETEROCYCLE AMIDE T-TYPE CALCIUM CHANNEL ANTAGONISTS<br/>[FR] ANTAGONISTES DES CANAUX CALCIQUES DE TYPE T À BASE D'AMIDE HÉTÉROCYCLIQUE
申请人:MERCK & CO INC
公开号:WO2009054983A1
公开(公告)日:2009-04-30
The present invention is directed to heterocycle amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
PhI(OAc)2-Mediated Regioselective Synthesis of 5-Guanidino-1,2,4-thiadiazoles and 1,2,4-Triazolo[1,5-a]pyridines via Oxidative N–S and N–N Bond Formation
construction of biologically important 5-guanidino-1,2,4-thiadiazole and 1,2,4-triazolo[1,5-a]pyridine derivatives has been developed. This new protocol involves the phenyliodine(III) diacetate [PhI(OAc)2]-mediated oxidative cyclization of thioureas/2-aminopyridines and imidates via N–S and N–N bond formation at ambient temperature. This method furnishes the versatile 5-guanidino-1,2,4-thiadiazoles and 1
PYRAZINYL AMIDE-T TYPE CALCIUM CHANNEL ANTAGONISTS
申请人:Barrow James C.
公开号:US20100216816A1
公开(公告)日:2010-08-26
The present invention is directed to pyrazinyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
The present invention is directed to heterocycle amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.