Driving Recursive Dehydration by P<sup>III</sup>/P<sup>V</sup> Catalysis: Annulation of Amines and Carboxylic Acids by Sequential C–N and C–C Bond Formation
作者:Morgan Lecomte、Jeffrey M. Lipshultz、Shin-Ho Kim-Lee、Gen Li、Alexander T. Radosevich
DOI:10.1021/jacs.9b06277
日期:2019.8.14
A method for the annulation of amines and carboxylicacids to form pharmaceutically relevant azaheterocycles via organophosphorus PIII/PV redox catalysis is reported. The method employs a phosphetane catalyst together with a mild bromenium oxidant and terminal hydrosilane reductant to drive successive C–N and C–C bond-forming dehydration events via the serial action of a catalytic bromophosphonium
Synthesis of a small library of phenylalkylamide derivatives as melatoninergic ligands for human mt 1 and MT 2 receptors
作者:Cécile Pégurier、Sophie Curtet、Jean-Paul Nicolas、Jean A. Boutin、Philippe Delagrange、Pierre Renard、Michel Langlois
DOI:10.1016/s0968-0896(99)00285-0
日期:2000.1
108 compounds was then synthesised from 12 arylalkyl amines and nine carboxylic acids. The compound mixtures were evaluated on chicken brain melatonin and recombinant human mt1 and MT2 receptors. Deconvolution of the most potent mixture demonstrated the superiority of 3-methoxy and 2,5-dimethoxy substitution on the phenyl ring with isopropyl, propyl and ethyl amido chains. Several compounds with nanomolar
inhibition at 1 x 10(3) mol ratio/TPA). These alkaloids were more active than the naturally occurring alkaloids, 23, 25, 33, 53, and 54. In addition, fifteen simpleisoquinolines, eighteen 1-benzylisoquinolines and eight protoberberines were evaluated with respect to their ability to scavenge 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radicals. Nine simpleisoquinolines, ten 1-benzylisoquinolines, and four protoberberines
The present invention relates to 3,4-dihydroisoquinolinium salt derivatives. More specifically, the present invention relates to 3,4-dihydroisoquinolinium salt derivatives of the following chemical formula (I).