A compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
A cationic Ir(I)–tolBINAP complex catalyzed an enantioselective C–C bond formation, which was initiated by secondary sp3 C–H bondcleavage adjacent to nitrogen atom. A wide variety of 2-(alkylamino)pyridines and alkenes were selectively transformed into the corresponding chiral amines with moderate to almost perfect enantiomeric excesses. Alkynes were also investigated as coupling partners. The effect
[EN] DERIVATIVES OF PIPERLONGUMINE AND USES THEREOF<br/>[FR] DÉRIVÉS DE PIPERLONGUMINE ET LEURS UTILISATIONS
申请人:AURANSA INC
公开号:WO2019103897A1
公开(公告)日:2019-05-31
The present invention relates to a group of 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3- dihydropyridin-6-one (piperlongumine) derivatives, analogs and pharmaceutically acceptable salts thereof. The present invention also relates to processes for preparing the same; a pharmaceutical composition and formulation containing a derivative of piperlogumine; and use of the derivatives and analogs for treating cancer.
The synthesis of a series of 2-(alkylamino)pyridines (1) in three steps from 2-aminopyridine (4) is reported. The products were obtained in 67-91% overall yield from 4.
ASYMMETRIC REDUCTION OF PROCHIRAL CYCLIC KETONES WITH LITHIUM ALUMINUM HYDRIDE PARTIALLY DECOMPOSED BY (1R,2S)-(−)-<i>N</i>-METHYLEPHEDRINE AND 2-ALKYLAMINOPYRIDINE
The title chiral hydride was found to reduce prochiral cyclicketones, affording the corresponding optically active cyclic alcohols in high optical(max. 9 8%ee) yields.