74116-68-0Relevant academic research and scientific papers
6π-Electrocyclization in water: microwave-assisted synthesis of polyheterocyclic-fused quinoline-2-thiones
Chen, Xiao-Lan,Li, Xiao-Yun,Liang, Xing-Xing,Liu, Yan,Lu, Xin-Yuan,Qu, Ling-Bo,Wei, Chuan-Wan,Yu, Bing,Zhu, Shan-Shan
supporting information, p. 4445 - 4449 (2020/08/10)
Microwave-assisted synthesis of polyheterocyclic-fused quinoline-2-thiones through the annulation of ortho-heteroaryl anilines and CS2 was realized in water without using any catalysts and additives. The desired products were obtained in high yields throu
Development of a novel class of pyrrolo-[1,2,5]benzothiadiazepine derivatives as potential anti-schistosomal agents
Chen, Jinglei,Sun, Weizhen,Yang, Jingjing,Sun, Huan,Wang, Zhixia,Dong, Lanlan,Qiao, Chunhua,Xia, Chao-Ming
, p. 3785 - 3787 (2013/07/25)
Analogues of pyrrolo-[1,2,5]benzothiadiazepine were prepared and evaluated against Schistosoma japonica. The biological data revealed that most benzothiazepine derivatives show anti-schistosomal activity to some extent, while α-chloronation of the title compound and another bioisosteric derivative pyrrolo-[1,2,5]benzodiazepine displayed the most distinct worm killing activity. This study proved that benzodiazepine may serve as a novel structural skeleton for the development of anti-schistosomal agents.
First enantioselective synthesis of aptazepine
Roszkowski, Piotr,Maurin, Jan K.,Czarnocki, Zbigniew
experimental part, p. 241 - 246 (2012/03/26)
Aptazepine (2-methyl-1,3,4,14b-tetrahydro-2H,10H-pyrazino[1,2-a]pyrrolo[2, 1-c][1,4]benzodiazepine), a potent tetracyclic antidepressant, was synthesized in both its enantiopure forms by using an asymmetric transfer hydrogenation in a key step. Reduction of the prochiral imine 7 gave the products (R)- and (S)-8 in 63% and 61% ee, respectively, but a single crystallization improved the enantiomeric purity to 98% ee. The final (R)- and (S)-aptazepines were prepared in four subsequent steps. The absolute configuration of intermediate (S)-8 was determined by X-ray crystallography. Georg Thieme Verlag Stuttgart · New York.
Iridium catalyzed asymmetric hydrogenation of cyclic imines of benzodiazepinones and benzodiazepines
Gao, Kai,Wu, Bo,Yu, Chang-Bin,Chen, Qing-An,Ye, Zhi-Shi,Zhou, Yong-Gui
supporting information; experimental part, p. 3890 - 3893 (2012/09/22)
Highly enantioselective Ir-catalyzed hydrogenation of seven-membered cyclic imines of benzodiazepinones and benzodiazepines was achieved with up to 96% ee. This method provides a direct access to synthesize a range of chiral cyclic amines existing in nume
Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan
Molinari, Albert J.,Trybulski, Eugene J.,Bagli, Jehan,Croce, Susan,Considine, John,Qi, Jian,Ali, Kadum,DeMaio, William,Lihotz, Lynne,Cochran, David
, p. 5796 - 5800 (2008/09/21)
Small molecule agonists and antagonists of the V2-vasopressin receptor have been discovered and have undergone clinical trials. In conjunction with these discovery programs, the synthesis and biological testing of various metabolites associated with these clinical targets were actively pursued. We now report the results of our synthetic efforts and the corresponding biological data generated for several of the metabolites of WAY-151932 and CL-347985 (Lixivaptan).
5H-Pyrrolo[2,1-c][1,4]benzodiazepine derivatives
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, (2008/06/13)
This disclosure describes substituted 11-piperazinyl-5H-pyrrolo[2,1-c][1,4]benzodiazepines useful as anti-psychotic or neuroleptic agents.
