Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones as 5-HT2C receptor agonists
摘要:
A series of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones is described, several examples of which exhibit potent 5-HT2C agonism with excellent selectivity over the closely related 5-HT2A and 5-HT2B receptors. Compounds such as 38 and 44 were shown to be effective in reducing food intake in an acute rat feeding model. (C) 2012 Elsevier Ltd. All rights reserved.
2-Substituted and 4-substituted aryl nitrone compounds
申请人:Kelly G. Michael
公开号:US20050182060A1
公开(公告)日:2005-08-18
The present invention provides aryl nitrones, compositions comprising the same and methods of their use for the treatment or prevention of oxidative, ischemic, ischemia/reperfusion-related and chemokine mediated conditions.
To develop a highly safe measure to treat Alzheimer's disease using a secretase-inhibiting substance, there is provided a compound represented by the following general formula (I) or a salt thereof:
wherein A represents a phenyl group or the like, R
1
represents a chlorine atom, a bromine atom, or a nitro group or the like, R
2
, R
3
, R
4
, and R
5
each represent a hydrogen atom or the like, and L represents CH
2
—CH
2
or CH═CH.
Copper catalyzed cross-coupling reactions of carboxylic acids: an expedient route to amides, 5-substituted γ-lactams and α-acyloxy esters
作者:S. Priyadarshini、P. J. Amal Joseph、M. Lakshmi Kantam
DOI:10.1039/c3ra41000e
日期:——
A convenient and recyclable catalytic protocol for the synthesis of N,N-dimethyl substituted amides, 5-substituted γ-lactams and α-acyloxy ethers from carboxylic acids using CuO nanoparticles and TBHP is described.
The first example of Cu(ii)-mediated oxidative coupling of aromatic carboxylic acids with the C(sp3)–H bond adjacent to the keto group ofN,N-dialkylamides has been developed.
Building bridges: We have developed an unprecedented asymmetricdecarbonylativearyladdition of an aromaticaldehyde to bicyclicalkenes, catalyzed by chiral cationiciridium. This process provides efficient access to a wide variety of enantioenriched bridged bicyclic systems from aromaticaldehydes in high yields and with excellent enantioselectivities (up to 90 % yield and up to 99 % ee).