197239-59-1Relevant articles and documents
Synthesis of Azepino[1,2-a]indole-10-amines via [6+1] Annulation of Ynenitriles with Reformatsky Reagent
Iioka, Ryoya,Yorozu, Kohei,Sakai, Yoko,Kawai, Rika,Hatae, Noriyuki,Takashima, Katsuki,Tanabe, Genzoh,Wasada, Hiroaki,Yoshimatsu, Mitsuhiro
supporting information, p. 1553 - 1558 (2021/02/26)
Lewis acid-catalyzed [6+1] annulation reactions of 2-cyano-1-propargyl- and 2-alkynyl-1-cyanomethyl-indoles with Reformatsky reagent are described. 8-Aryl, 8-alkyl-, 8-hetaryl-, 9-aryl, and 9-alkyl-azepino[1,2-a]indole amines were obtained through a 7-endo-mode cyclization of the β-aminoacrylate intermediates. The antiproliferative activity of the azepino[1,2-a]indoles analogs against the HCT-116 cells were also examined.
Catalyst-Free Annulation of 2-Pyridylacetates and Ynals with Molecular Oxygen: An Access to 3-Acylated Indolizines
Chen, Zhengwang,Liang, Pei,Ma, Xiaoyue,Luo, Haiqing,Xu, Guohai,Liu, Tanggao,Wen, Xiaowei,Zheng, Jing,Ye, Hui
supporting information, p. 1630 - 1639 (2019/01/26)
A catalyst and additive-free annulation of 2-pyridylacetates and ynals under molecular oxygen was the first developed, affording 3-acylated indolizines in good to excellent yields. Molecular oxygen was used as the source of the carbonyl oxygen atom in indolizines. This approach was compatible with a wide range of functional groups, and especially it has been successfully extended to unsaturated double bonds and triple bonds, which were difficult to prepare by previous methods in a single step.
1-(1,2,5-thiadiazol-4-yl)-4-azatricyclo[2.2.1.02,6]heptanes as new potent muscarinic M1 agonists: Structure-activity relationship for 3-aryl- 2-propyn-1-yloxy and 3-aryl-2-propyn-1-ylthio derivatives
Jeppesen, Lone,Olesen, Preben H.,Hansen, Lena,Sheardown, Malcolm J.,Thomsen, Christian,Rasmussen, Th?ger,Jensen, Anders Fink,Christensen, Michael S.,Rimvall, Karin,Ward, John S.,Whitesitt, Celia,Calligaro, David O.,Bymaster, Frank P.,Delapp, Neil W.,Felder, Christian C.,Shannon, Harlan E.,Sauerberg, Per
, p. 1999 - 2006 (2007/10/03)
Two new series of 1-(1,2,5-thiadiazol-4-yl)-4- azatricyclo[2.2.1.02,6]heptanes were synthesized and evaluated for their in vitro activity in cell lines transfected with either the human M1 or M2 receptor. 3-Phenyl-2-propyn-1-yloxy and -1-ylthio analogues substituted with halogen in the meta position showed high functional potency, efficacy, and selectivity toward the M1 receptor subtype. A quite unique functional M1 receptor selectivity was observed for compounds 8b, 8d, 8f, 9b, 9d, and 9f. Bioavailability studies in rats indicated an oral bioavailability of about 20-30%, with the N-oxide as the only detected metabolite.
