71936-92-0Relevant academic research and scientific papers
A Modular Approach to Dibenzo-fused ?-Lactams: Palladium-Catalyzed Bridging-C?H Activation
Huang, Xueliang,Ma, Liyao,Xia, Jiajin,Xin, Luoting,Yu, Yinghua,Zhu, Lei
supporting information, p. 18261 - 18266 (2020/08/21)
Tricyclic ring systems possessing a dibenzo structure joined to a seven-membered heterocyclic ring frequently show important biological activities. However, a modular approach to these molecules based on efficient intermolecular reaction of readily available chemicals is lacking. Herein, an unprecedented palladium-catalyzed formal [4+3] annulation for modular construction of these tricyclic systems is described. This reaction features easily accessible reactants (o-haloarylaldehydes and N-tosylhydrazones), broad substrate scope, and excellent functional group compatibility. The synthetic potential is demonstrated by the easy scale-up reactions, late-stage modification of complex molecules, and collective synthesis of bioactive molecules and approved drugs.
The enantioselective synthesis of (S)-(+)-mianserin and (S)-(+)-epinastine
Roszkowski, Piotr,Maurin,Czarnocki, Zbigniew
, p. 1509 - 1513 (2016/04/09)
A simple enantioselective synthetic procedure for the preparation of mianserin and epinastine in optically pure form is described. The key step in the synthetic pathway is the asymmetric reduction of the cyclic imine using asymmetric transfer hydrogenation conditions.
Hybrid approach for the design of highly affine and selective dopamine D3 receptor ligands using privileged scaffolds of biogenic amine GPCR ligands
Sasse, Britta C.,Mach, Ulrich R.,Leppaenen, Jukka,Calmels, Thierry,Stark, Holger
, p. 7258 - 7273 (2008/03/27)
A series of compounds containing privileged scaffolds of the known histamine H1 receptor antagonists cetirizine, mianserin, ketotifen, loratadine, and bamipine were synthesized for further optimization as ligands for the related biogenic amine binding dopamine D3 receptor. A pharmacological screening was carried out at dopamine D2 and D3 receptors. In the preliminary testing various ligands have shown moderate to high affinities for dopamine D3receptors, for example, N-(4-{4-[benzyl(phenyl)amino]piperidin-1-yl}butylnaphthalen-2-carboxamide (19a) (hD3 Ki = 0.3 nM; hD2 Ki = 703 nM), leading to a selectivity ratio of 2343.
1,2,3,4,10,14b-hexahydrodibenzo[c,f]pyrazino-[1,2-a]azepino derivatives and 10-aza, 10-oxa and 10-thia analogues
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, (2008/06/13)
STR1 A compound of general formula (I), wherein X=CH2, O, S or NR4, and Y=formula (II): where R1 =H, lower alkyl or an aryloxyalkyl group, wherein the aryl group is optionally substituted by alkyl, alkoxy, hydrogen, alkyl substituted by hydrogen, and n is an integer between 0 and 5, and Z=O, S or NR2 ; wherein R2 =H, lower alkyl, hydroxy, amino cyano or acyl, R3 =H, or lower alkyl, and R4 =H, lower alkyl, or lower acyl, and pharmaceutically acceptable salts thereof.
