The present invention relates to compounds of formula (I),
wherein
R
1
is heteroaryl or heterocyclyl, optionally substituted;
R
2
is C
1-4
alkyl, heterocyclyl, C
1-4
alkylaryl, C
1-4
alkylheteroaryl, carbocyclyl, C
1-4
alkylheterocyclyl, heterocyclyl-heteroaryl, aryl-heterocyclyl, carbocyclyl-heteroaryl, heterocyclyl-aryl, optionally substituted;
R
3
is hydrogen or C
1-4
alkyl, or
R
2
and R
3
may together with the nitrogen atom, form a saturated ring system containing 4, 5 or 6 ring forming atoms, and optionally substituted;
R
4
is hydrogen, halogen, methyl or methoxy;
to pharmaceutical composition containing said compounds and to the use of said compounds in therapy, for instance in treating cognitive disorders.
The present invention further relates to new intermediates useful in the preparation thereof.
A novel enantioselective protonation protocol that is triggered by reductive cross coupling of olefins is reported. When under cooperative photoredox and chiral hydrogen-bonding catalytic conditions and using a terminal reductant, various α-branched vinylketones with diverse vinylazaarenes could provide important enantioenriched azaarene derivatives containing tertiary stereocenters at their remote
Visible light-promoted umpolung coupling of aryl tri-/difluoroethanones with 2-alkenylpyridines
作者:Xiao Xu、Qing-Qiang Min、Na Li、Feng Liu
DOI:10.1039/c8cc06748a
日期:——
Tertiaryalcohols bearing a trifluoromethyl group are of considerable medicinal interest. Using an umpolung strategy, we herein report the first intermolecular reductive cross-coupling of aryl tri-/difluoroethanones with 2-alkenylpyridines with the aid of a Brønsted acid catalyst upon visible-light irradiation. This metal-free reaction is operationally simple and performed at ambient temperature, allowing
Catalytic Enantioselective Addition of Prochiral Radicals to Vinylpyridines
作者:Kangning Cao、Siu Min Tan、Richmond Lee、Songwei Yang、Hongshao Jia、Xiaowei Zhao、Baokun Qiao、Zhiyong Jiang
DOI:10.1021/jacs.9b00286
日期:2019.4.3
Pyridine, one of the most important azaarenes, is ubiquitous in functional molecules. The electronic properties of pyridine have been exploited to trigger asymmetric transformations of prochiral species as a direct approach for accessing chiral pyridine derivatives. However, the full potential of this synthetic strategy for the construction of enantioenriched γ-functionalized pyridines remains untapped
ORGANOSILICON COMPOUND, MAKING METHOD, ADHESIVE COMPOSITION, AND ARTICLE
申请人:Shin-Etsu Chemical Co., Ltd.
公开号:US20150099414A1
公开(公告)日:2015-04-09
An organosilicon compound having a hydrolyzable silyl group and pyridine ring in the molecule is provided. A composition comprising a polymer having an isocyanate, epoxy or acid anhydride in admixture with the organosilicon compound is shelf stable.