Palladium-Catalyzed Amination of Aryl Bromides Utilizing Arene−Chromium Complexes as Ligands
摘要:
The arene-chromium complexes of o-diphenylphosphino alpha-phenylethylamine or a-phenylethyl methyl ether derivatives were examined with regard to their activity as ligands for palladium(0)-catalyzed aryl amination of aryl bromides with a variety of amines. Both steric and electronic factors were found to be significant for the efficient palladium-catalyzed aryl amination reactions. Modulation of the inductive capacity of the arylphosphine atom was achieved by photoinduced ligand exchange of one carbonyl of the chromium tripode in the presence of electron-donating triphenylphosphine or phosphite. Among these arene-chromium ligands, the use of the monophosphineor monophosphite-(dicarbonyl)chromium of N,N-dimethyl alpha-(o-diphenylphosphino)phenylethylamine and methyl alpha-(o-diphenylphosphino)phenylethyl ether produced the palladium(0)-catalyzed aryl amination products with cyclic amines or acyclic secondary amines in high yields; the corresponding strong electron-withdrawing tricarbonylchromium complex resulted in a modest yield of the aryl amination.
The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
METHODS AND FLUORINATED COMPOSITIONS FOR TREATING AMYLOID-RELATED DISEASES
申请人:Neurochem (International) Limited
公开号:EP1828111A2
公开(公告)日:2007-09-05
US8258306B2
申请人:——
公开号:US8258306B2
公开(公告)日:2012-09-04
[EN] METHODS AND FLUORINATED COMPOSITIONS FOR TREATING AMYLOID-RELATED DISEASES<br/>[FR] PROCEDES ET COMPOSITIONS FLUOREES POUR LE TRAITEMENT DE MALADIES ASSOCIEES AUX AMYLOIDES
申请人:NEUROCHEM INT LTD
公开号:WO2006059252A2
公开(公告)日:2006-06-08
[EN] Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease. Also described are methods, compounds, pharmaceutical compositions and kits for detecting, diagnosing, monitoring and treating or preventing amyloid-related disease. [FR] L'invention concerne des procédés, des composés, des compositions pharmaceutiques et des kits destinés au traitement ou à la prévention de maladies associées aux amyloïdes. L'invention concerne également des procédés, des composés, des compositions pharmaceutiques et des kits destinés à la détection, au diagnostic, au contrôle et au traitement ou à la prévention de maladies associées aux amyloïdes.
Palladium-Catalyzed Amination of Aryl Bromides Utilizing Arene−Chromium Complexes as Ligands
作者:Ken Kamikawa、Suguru Sugimoto、Motokazu Uemura
DOI:10.1021/jo981327+
日期:1998.11.1
The arene-chromium complexes of o-diphenylphosphino alpha-phenylethylamine or a-phenylethyl methyl ether derivatives were examined with regard to their activity as ligands for palladium(0)-catalyzed aryl amination of aryl bromides with a variety of amines. Both steric and electronic factors were found to be significant for the efficient palladium-catalyzed aryl amination reactions. Modulation of the inductive capacity of the arylphosphine atom was achieved by photoinduced ligand exchange of one carbonyl of the chromium tripode in the presence of electron-donating triphenylphosphine or phosphite. Among these arene-chromium ligands, the use of the monophosphineor monophosphite-(dicarbonyl)chromium of N,N-dimethyl alpha-(o-diphenylphosphino)phenylethylamine and methyl alpha-(o-diphenylphosphino)phenylethyl ether produced the palladium(0)-catalyzed aryl amination products with cyclic amines or acyclic secondary amines in high yields; the corresponding strong electron-withdrawing tricarbonylchromium complex resulted in a modest yield of the aryl amination.