Redox-Triggered Switchable Synthesis of 3,4-Dihydroquinolin-2(1<i>H</i>)-one Derivatives via Hydride Transfer/<i>N</i>-Dealkylation/<i>N</i>-Acylation
作者:Xiaoyu Yang、Liang Wang、Fangzhi Hu、Lubin Xu、Sanming Li、Shuai-Shuai Li
DOI:10.1021/acs.orglett.0c03863
日期:2021.1.15
The switchable synthesis of 3-non, 3-mono, 3,3′-disubstituted 3,4-dihydroquinolin-2(1H)-ones was developed through a redox-neutral hydride-transfer/N-dealkylation/N-acylation strategy from o-aminobenzaldehyde with 4-hydroxycoumarin, and Meldrum’s acid, respectively. The unprecedented strategy for the synthesis of 3,3′-highly functionalized 3,4-dihydroquinolin-2(1H)-one has been realized with the in
[EN] MITOGEN ACTIVATED PROTEIN KINASE-ACTIVATED PROTEIN KINASE-2 INHIBITING COMPOUNDS<br/>[FR] COMPOSES INHIBANT LA PROTEINE KINASE-2 ACTIVEE PAR LA PROTEINE KINASE ACTIVEE PAR DES AGENTS MITOGENES
申请人:PHARMACIA CORP
公开号:WO2004058762A1
公开(公告)日:2004-07-15
Compounds are described which inhibit mitogen activated protein kinase-activated protein kinase-2 (MK-2). Methods of using such compounds for the inhibition of MK-2, and for the prevention or treatment of a disease or disorder that is mediated by TNFα, are described, where the method involves administering to the subject an MK-2 inhibiting compound of the present invention. Therapeutic compositions, pharmaceutical compositions and kits which contain the present MK-2 inhibiting compounds are also described.
The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula:
wherein R
1
represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R
2
represents a group —OR
3
or the like, and R
3
represents a hydrogen atom, C1-C6 alkyl group or the like, or R
1
and —(CH
2
)
n
R
2
may bind to each other together with carbon atoms adjacent thereto through nitrogen atoms so as to form a spiro ring represented by the general formula (H):
wherein R
41
is hydrogen, C1-C6 alkyl group or the like. The present compound has an excellent bactericidal action against
Mycobacterium tuberculosis
, multi-drug-resistant
Mycobacterium tuberculosis
, and atypical acid-fast bacteria.