N6-SUBSTITUTED ADENOSINE DERIVATIVES AND N6-SUBSTITUTED ADENINE DERIVATIVES AND USES THEREOF
申请人:Shi Jiangong
公开号:US20130045942A1
公开(公告)日:2013-02-21
The present invention provides N
6
-substituted adenosine derivatives and N
6
-substituted adenine derivatives, manufacturing methods thereof, a pharmaceutical composition comprising the said compounds above, and uses of these compounds in manufacturing medicaments and health-care products for treating insomnia, convulsion, epilepsy, and Parkinson's diseases, and preventing and treating dementia.
Synthesis of α-Substituted Primary Benzylamines through Copper-Catalyzed Cross-Dehydrogenative Coupling
作者:Søren Kramer
DOI:10.1021/acs.orglett.8b03505
日期:2019.1.4
A copper-catalyzed route to α-substituted, primarybenzylamines by C–H functionalization of alkylarenes is described. The method directly affords the amine hydrochloride salt. Catalyst loadings down to 0.1 mol % in combination with scalability, insensitivity to air and moisture, and no need for column chromatography makes the procedure highly practical. The facile synthesis of the racemate of a blockbuster
The benzylic proton of alkylarenes 1 was replaced by an azido group in one step by reaction with trimethylsilyl azide or hydrazoic acid in chloroform in the presence of 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ). The 1-arylalkyl azides 2 were reduced to amines 3, which were characterized as their hydrochlorides 4.
Chiral Brønsted Acids Catalyze Asymmetric Additions to Substrates that Are Already Protonated: Highly Enantioselective Disulfonimide-Catalyzed Hantzsch Ester Reductions of NH–Imine Hydrochloride Salts
作者:Benjamin List、Vijay N. Wakchaure、Carla Obradors
DOI:10.1055/s-0040-1706413
日期:2020.10
are frequently used substrates in asymmetric Bronsted acid catalysis, their corresponding salts are generally considered unsuitable reaction partners. Such processes are challenging because they require the successful competition of a catalytic amount of a chiral anion with a stoichiometric amount of an achiral one. We now show that enantiopure disulfonimides enable the asymmetric reduction of N–H imine