51908-64-6Relevant articles and documents
Facile Synthesis of 2-Aminocyclobutenylphosphonates
Al Quntar, A. A. A.,Dembitsky, V.,Dweik, H.
, p. 137 - 142 (2020)
The addition of various amines to diethyl 4-chlorobut-1-yn-1-ylphosphonate produced novel biologically potent substituted diethyl 2-aminocyclobut-1-en-1-ylphosphonates in 70–83% isolated yield. This regioselective reaction was carried out at room temperat
Synthesis of the ortho / meta / para isomers of relevant pharmaceutical compounds by coupling a Sonogashira reaction with a regioselective hydration
Leyva-Perez, Antonio,Cabrero-Antonino, Jose R.,Rubio-Marques, Paula,Al-Resayes, Saud I.,Corma, Avelino
, p. 722 - 731 (2014/04/03)
Aryl ketones substituted in ortho, meta, and para position are prepared by a palladium-catalyzed Sonogashira reaction followed by a regioselective hydration of the so-formed alkyne with triflimidic acid or a gold catalyst, under catalytic conditions. This methodology opens a way to obtain substituted aryl alkyl ketones from readily available starting materials, haloarenes, and terminal alkynes. The syntheses of the different regioisomers of haloperidol, melperone, pipamperone, and ibuprofen are presented. Structure-activity relationships for these compounds are studied with dopaminergic and cyclooxigenase binding assays.
Copper-catalyzed asymmetric 1,4-addition of alkenyl alanes to N-substituted-2-3-dehydro-4-piperidones
Mueller, Daniel,Alexakis, Alexandre
supporting information; experimental part, p. 1842 - 1845 (2012/06/18)
Readily available vinyl alanes are used in the Cu-catalyzed asymmetric conjugate addition reaction to N-substituted-2-3-dehydro-4-piperidones. The enhanced reactivity of recently developed and easily prepared phosphine amine ligands in combination with inexpensive Cu(II)naphtenate (CuNp) allows the introduction of a great variety of alkenyl, alkyl, and aryl aluminums in high enantioselectivity.