New ligands for the ORL-1 receptor are described, useful for antagonising the activity of said receptors in a patient in need thereof, and for preventing and treating illnesses dependent on the activation of this receptor. The new compounds conform to structural formula (I) wherein R1, R2, R3, R4 are further defined in the description.
作者:Bruce W. Horrom、Morris Freifelder、George R. Stone
DOI:10.1021/ja01608a061
日期:1955.2.1
An organophotocatalytic late-stage N–CH<sub>3</sub> oxidation of trialkylamines to <i>N</i>-formamides with O<sub>2</sub> in continuous flow
作者:Mark John P. Mandigma、Jonas Žurauskas、Callum I. MacGregor、Lee J. Edwards、Ahmed Shahin、Ludwig d'Heureuse、Philip Yip、David J. S. Birch、Thomas Gruber、Jörg Heilmann、Matthew P. John、Joshua P. Barham
DOI:10.1039/d1sc05840a
日期:——
We report an organophotocatalytic, N–CH3-selective oxidation of trialkylamines in continuous flow. Based on the 9,10-dicyanoanthracene (DCA) core, a new catalyst (DCAS) was designed with solubilizing groups for flow processing. This allowed O2 to be harnessed as a sustainable oxidant for late-stage photocatalytic N–CH3 oxidations of complex natural products and active pharmaceutical ingredients bearing
我们报道了连续流中三烷基胺的有机光催化、N-CH 3选择性氧化。基于9,10-二氰基蒽( DCA )核心,设计了一种带有增溶基团的流动处理新型催化剂( DCAS )。这使得 O 2可以作为一种可持续的氧化剂,用于复杂天然产物和带有先前方法无法耐受的官能团的活性药物成分的后期光催化 N-CH 3氧化。有机光催化气液流动过程比间歇模式提供更清洁的反应,停留时间短,为 13.5 分钟,生产率高达每天 0.65 克。光谱和计算机理研究表明,与难溶性DCA相比,催化剂衍生化不仅提高了新催化剂的溶解度,而且深刻地将光催化机制从单线态电子转移 (SET) 胺还原猝灭转向能量转移 (E n T)氧2 。