700856-05-9Relevant academic research and scientific papers
Late Stage Functionalization of Secondary Amines via a Cobalt-Catalyzed Electrophilic Amination of Organozinc Reagents
Gra?l, Simon,Chen, Yi-Hung,Hamze, Clémence,Tüllmann, Carl Phillip,Knochel, Paul
, p. 494 - 497 (2019/01/14)
A general preparation of polyfunctional hydroxylamine benzoates from the corresponding secondary amines is reported. This convenient synthesis allows the setup of a late-stage functionalization of various secondary amines, including pharmaceuticals and peptidic derivatives. Thus, a cross-coupling of hydroxylamine benzoates with various alkyl-, aryl-, and heteroaryl-zinc chlorides in the presence of 5 mol % CoCl2 (25 °C, 2 h) provides a range of polyfunctional tertiary amines. This method was used to prepare penfluridol and gepirone.
Morpholylureas are a new class of potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase (AKR1C3)
Flanagan, Jack U.,Atwell, Graham J.,Heinrich, Daniel M.,Brooke, Darby G.,Silva, Shevan,Rigoreau, Laurent J.M.,Trivier, Elisabeth,Turnbull, Andrew P.,Raynham, Tony,Jamieson, Stephen M.F.,Denny, William A.
, p. 967 - 977 (2014/02/14)
Inhibitors of the aldo-keto reductase enzyme AKR1C3 are of interest as potential drugs for leukemia and hormone-related cancers A series of non-carboxylate morpholino(phenylpiperazin-1-yl)methanones were prepared by palladium-catalysed coupling of substit
