New ligands for the ORL-1 receptor are described, useful for antagonising the activity of said receptors in a patient in need thereof, and for preventing and treating illnesses dependent on the activation of this receptor. The new compounds conform to structural formula (I) wherein R1, R2, R3, R4 are further defined in the description.
A novel and unusual method for C–N bond formation in 1-substituted-pyrrolidin-2-ones
作者:Neelima Sinha、Sanjay Jain、Nitya Anand
DOI:10.1016/j.tetlet.2004.10.162
日期:2005.1
A novel 5-C-N bond forming reaction is reported, which involves heating 1-substituted-pyrrolidin-2-ones with cyclic amines in the presence of a base. This reaction provides a convenient method for the synthesis of 1,5-disubstituted-pyrrolidin-2-ones. (C) 2004 Elsevier Ltd. All rights reserved.
US5776936A
申请人:——
公开号:US5776936A
公开(公告)日:1998-07-07
US7157464B2
申请人:——
公开号:US7157464B2
公开(公告)日:2007-01-02
Copper catalyzed <i>N</i>-formylation of α-silyl-substituted tertiary <i>N</i>-alkylamines by air
作者:Yichao Zhao、Lachlan David Bruce、Jianwen Jin、Bo Xia、Philip Wai Hong Chan
DOI:10.1039/d0gc01242d
日期:——
Moreover, it delinates a ligand- and additive-free amine oxidation process mediated by a low-cost metal salt with oxygen from air taking on the role of both the terminal oxidant and as part of the formylation reagent, which is unprecedented in copper catalysis. It also offers the first synthetic method that can selectively generate α-amino radical species as reactive intermediates from α-silylamines under