substituted N-aryl-2-cyanoazetidines based on an anionic ring-closure reaction. These compounds can be prepared from β-amino alcohols in enantiomerically pure form through a three-step sequence involving (i) copper-catalyzed N-arylation, (ii) N-cyanomethylation of the secondary aniline, and (iii) one-pot mesylation followed by ring closure induced by a base. This high-yielding sequence gives access to azetidines
Improved synthetic method of Benzo[a]pheno-selenazinium phototherapeutic agents
作者:Xiuxiu Yue、Jing Xu、Xiaozhong Liu、Xiangzhi Song、James W. Foley
DOI:10.1016/j.dyepig.2021.109154
日期:2021.4
Benzo[a]phenoselenazinium dyes are excellent photodynamic therapeutic agents that have a red absorption (660 nm), high singlet oxygen quantum yield (>0.8), and good water-solubility and liposolubility. Bis-(3-diethylaminophenyl) diselenide, the most important intermediate for the synthesis of benzo[a]phenoselenazinium dyes, is previously prepared in one pot through 3 steps, during which special care
苯并[ a ]酚硒氮鎓染料是出色的光动力学治疗剂,具有红色吸收(660 nm),高单线态氧量子产率(> 0.8)以及良好的水溶性和脂溶性。双-(3-二乙基氨基苯基)二硒化物是合成苯并[ a ]酚硒基氮鎓染料的最重要中间体,以前需要在一锅中分三步进行制备,在此期间需要格鲁纳德试剂和有毒硒蒸气的制备。在这项工作中,我们使用CuO纳米粉将卤代苯胺与硒直接偶联,在温和的条件下以高产率获得纯的双-(3-二乙基氨基苯基)二硒化物(一步法),而无需柱色谱法。四种苯并[ a ]苯硒基氮鎓染料,使用改进的合成方法可以容易地制备5a-d;并研究了它们在活细胞中的光毒性。改进的方法可用于大规模合成苯并[ a ]苯并硒氮鎓染料,从而可能刺激这种光敏剂的光动力学研究。
The present invention relates to a compound of formula (I), or one of its pharmaceutically acceptable salts:
wherein R1, R2 and -X-Y- have specific definitions.
It also relates to the use of such a compound as reactivator of acetylcholinesterase for treating organophosphorous nerve agents poisoning; and to a process for preparing it.
The Acrylamide Moiety as an Activated Alkene Component in the Intramolecular Baylis-Hillman Reaction: Facile Synthesis of Functionalized α-Methylene Lactam and Spirolactam Frameworks
A facile strategy for the intramolecularBaylis–Hillmanreaction by utilizing an acrylamidemoiety as an activatedalkenecomponent was developed, which thus provides a convenient protocol for obtaining five- and six-membered α-methylenelactam and spirolactam derivatives.