5,7-二甲基-2-苯基-1-氧-1- H-吡唑并[1,2 - a ]吡唑-4-基-3-醇酸酯的微波辅助亲核裂解为α-苯基丙二酰胺
摘要:
在无溶剂微波条件下,通过选择性亲核裂解5,7-二甲基-2-苯基-1-氧-1- H-吡唑并[1,2 - a ]吡唑-4-基-3-醇酸酯制备了三种α-苯基丙二酰胺。合成。采用三种弱亲核体是苯胺,p -chloroaniline和米-甲苯胺。这三种苯胺衍生物的α-苯基丙二酰胺无法使用先前报道的溶剂通过3-氧代吡唑并[1,2 - a ]吡唑-8-基-1-油酸酯来制备。使用红外光谱,1 H nmr和电喷雾质谱对所有产品进行表征。起始吡唑并[[1,2-] a的单晶X射线结构]吡唑和α-phenylmalon-米-toluidide也报道。
N-(α-Ketoacyl)anthranilicacids were prepared by oxidative ring opening of 3-hydroxyquinoline-2,4(1H,3H)-diones by using paraperiodic acid (H5IO6) or sodium periodate (NaIO4). The optimisation of the reaction conditions is described as well as the utilisation of N-(α-ketoacyl)anthranilicacids in the preparation of anthranilicacid hydrochlorides.
cis-bromoiminolactones, electrochemical conditions exhibited complementarydiastereoselectivity to afford the trans-products. A variety of substituents on the nitrogen atoms and an α-position of the malonamide were tolerated under both sets of conditions to afford the corresponding iminolactones in excellent yields and high diastereoselectivities.
BRAEUNIGER; STENS, Pharmazie, 1963, vol. 18, p. 585 - 600
作者:BRAEUNIGER、STENS
DOI:——
日期:——
DE490274
申请人:——
公开号:——
公开(公告)日:——
3-Phenyl-4-hydroxyquinolin-2(1H)-ones: potent and selective antagonists at the strychnine-insensitive glycine site on the N-methyl-D-aspartate receptor complex
作者:Loretta A. McQuaid、Edward C. R. Smith、David Lodge、Etienne Pralong、James H. Wikel、David O. Calligaro、Patrick J. O'Malley