74116-68-0Relevant articles and documents
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
First enantioselective synthesis of aptazepine
Roszkowski, Piotr,Maurin, Jan K.,Czarnocki, Zbigniew
, 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.
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).