Catalytic N-Alkylation of Amines Using Carboxylic Acids and Molecular Hydrogen
作者:Iván Sorribes、Jose R. Cabrero-Antonino、Cristian Vicent、Kathrin Junge、Matthias Beller
DOI:10.1021/jacs.5b07994
日期:2015.10.28
green N-alkylation of amines has been accomplished by applying readily available carboxylic acids in the presence of molecular hydrogen. Applying an in situ formed ruthenium/triphos complex and an organic acid as cocatalyst, a broad range of alkylated secondary and tertiary amines are obtained in good to excellent yields. This novel method is also successfully applied for the synthesis of unsymmetrically
通过在分子氢存在下应用容易获得的羧酸,已经实现了胺的方便、实用和绿色的 N-烷基化。应用原位形成的钌/三磷配合物和有机酸作为助催化剂,可以以良好到极好的收率获得范围广泛的烷基化仲胺和叔胺。这种新方法还成功地应用于通过相应胺、羧酸和作为 C1 源的 CO2 的直接三组分偶联反应合成不对称取代的 N-甲基/烷基苯胺。
Novel benzylamine derivatives as CETP inhibitors
申请人:Baruah Anima
公开号:US20060178514A1
公开(公告)日:2006-08-10
The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.
This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I
The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABA
A
receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed.
This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABA
A
receptors in tissue sections.
Novel benzylamine derivatives and their utility as cholesterol ester-transfer protein inhibitors
申请人:Baruah Anima
公开号:US20070015758A1
公开(公告)日:2007-01-18
The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.
PYRAZOLE COMPOUNDS FOR TREATMENT OF NEURODEGENERATIVE DISORDERS
申请人:Chen L. Yuhpyng
公开号:US20070270474A1
公开(公告)日:2007-11-22
The invention provides compounds of Formula I:
wherein R
1
, R
2
, R
3
, R
4
, R
6
, R
7
, R
8
and A are as defined. Compounds of formula I have activity inhibiting production of Aβ-peptide. The invention also provides pharmaceutical compositions and methods for treating diseases, for example Alzheimer's disease, in mammals comprising compounds of Formula I.