220707-99-3Relevant academic research and scientific papers
Rhodium(i)-catalyzed Pauson-Khand-type reaction using formic acid as a CO surrogate: An alternative approach for indirect CO2 utilization
Lang, Xian-Dong,You, Fei,He, Xing,Yu, Yi-Chen,He, Liang-Nian
supporting information, p. 509 - 514 (2019/02/14)
Formic acid is found to be an ideal CO surrogate for the rhodium(i)-catalyzed Pauson-Khand-type (PK-type) reaction of various substituted 1,6-enynes to afford bicyclic cyclopentenones in moderate to good yields. High TON value of up to 263 and good results in the gram-scale experiment were also obtained, demonstrating the efficacy of this methodology. In addition, heterocyclic molecules of pharmaceutical importance were also furnished via inter- or intra-molecular hetero-PK-type reactions, further broadening the application of current strategy. In this protocol, formic acid was utilized as a bridging molecule for the conversion of CO2 to CO, since formic acid is manufactured via catalytic hydrogenation of CO2 and releases CO in the presence of acetic anhydride readily. Therefore, this methodology represents a green and indirect approach for chemical valorization of CO2 in the preparation of value-added compounds.
Palladium-Catalyzed Nitrile-Assisted C(sp3)-Cl Bond Formation for Synthesis of Dichlorides
He, Dandan,Huang, Liangbin,Li, Jianxiao,Wu, Wanqing,Jiang, Huanfeng
supporting information, p. 8308 - 8311 (2019/10/16)
A palladium-catalyzed coupling procedure of alkenes with alkynylnitriles has been demonstrated for the synthesis of dichlorides. The reaction is the first example of nitrile-assisted C(sp3)-Cl formation promoted by coordination of a cyano group with an alkylpalladium(II) complex. The construction of a five-membered cycle intermediate successfully inhibits the β-hydride abstraction, resulting in direct C-Cl bond reductive elimination of alkylpalladium(II) chloride.
AMINE COMPOUND AND PHARMACEUTICAL USE THEREOF
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Page/Page column 83, (2010/04/25)
Provided is a novel amine compound represented by the following formula (I) having a superior peripheral blood lymphocyte decreasing action and superior in the immunosuppressive action, rejection suppressive action and the like, which shows decreased side effects of, for example, bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof. wherein each symbol is as defined in the specification.
Gold(I)-catalyzed enantioselective ring expansion of allenylcyclopropanols
Kleinbeck, Florian,Toste, F. Dean
supporting information; experimental part, p. 9178 - 9179 (2009/12/06)
(Chemical Equation Presented) The asymmetric gold(I)-catalyzed ring expansion of 1-allenylcyclopropanols is described. The method provides synthetically valuable cyclobutanones with a vinyl-substituted quaternary stereogenic center in high enantioselectivities and yields. The method shows a broad substrate scope, tolerating protected alcohols and amines, alkenes, unsaturated esters, and acetals. The reaction is easily adjustable to large-scale synthesis, leading to product formation without significant loss of selectivity or yield with only 0.5 mol% catalyst loading.
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.
