Desulfonylation-Initiated Distal Alkenyl Migration in Copper-Catalyzed Alkenylation of Unactivated Alkenes
摘要:
A novel and efficient protocol for desulfonylation-initiated distal alkenyl migration and its application to the elusive alkenylation of unactivated alkenes have been presented. This radical cascade process has successfully achieved the vicinal difluoroalkylalkenylation of unactivated alkenes with excellent chemo-, regio-, and stereoselectivity in high efficiency under mild conditions. The reactions afford previously unknown 3,3-difluoro-S-styrylpiperidin-2-one derivatives or beta-styryl-gamma-difluoroalkyl amines bearing a quaternary stereocenter. This is the first report of difunctionalization of unactivated alkenes through desulfonylation-initiated distal alkenyl migration.
Desulfonylation-Initiated Distal Alkenyl Migration in Copper-Catalyzed Alkenylation of Unactivated Alkenes
摘要:
A novel and efficient protocol for desulfonylation-initiated distal alkenyl migration and its application to the elusive alkenylation of unactivated alkenes have been presented. This radical cascade process has successfully achieved the vicinal difluoroalkylalkenylation of unactivated alkenes with excellent chemo-, regio-, and stereoselectivity in high efficiency under mild conditions. The reactions afford previously unknown 3,3-difluoro-S-styrylpiperidin-2-one derivatives or beta-styryl-gamma-difluoroalkyl amines bearing a quaternary stereocenter. This is the first report of difunctionalization of unactivated alkenes through desulfonylation-initiated distal alkenyl migration.
Visible-Light-Induced Direct Oxidative C−H Amidation of Heteroarenes with Sulfonamides
作者:Kun Tong、Xiaodong Liu、Yan Zhang、Shouyun Yu
DOI:10.1002/chem.201604014
日期:2016.10.24
A direct oxidative C−H amidation of heteroarenes with sulfonamides via nitrogen‐centered radicals has been achieved. Nitrogen‐centered radicals are directly generated from oxidative cleavage of N−H bonds under visible‐light photoredox catalysis. Sulfonamides, which are easily accessed, are used as tunable nitrogen sources and bleach (aqueous NaClO solution) is used as the oxidant. A variety of heteroarenes
The present invention provides a novel compound having an antiviral action, in particular, an HIV replication inhibiting action, as well as a pharmaceutical composition, in particular, an anti-HIV agent.
wherein, a broken line means the presence or absence of a bond; R
1
is substituted or unsubstituted alkyl etc., R
2
is substituted or unsubstituted alkyloxy etc.; n is 1 or 2; R
3
is a substituted or unsubstituted aromatic carbocyclic group; R
4
is a hydrogen atom etc.; R
5
is a substituted or unsubstituted aromatic carbocyclic group etc.; Y is a single bond etc.; R
6
is substituted or unsubstituted alkyl; R
7
is —Z—R
71
etc.; Z is —NR
72
—CO— etc.; R
71
is substituted or unsubstituted alkyl etc.; R
72
is a hydrogen atom etc.
A compound represented by the following general formula (1) or a salt thereof, which has superior inhibitory activity against type 4 PLA
2
, and thus has prostaglandin and/or leucotriene production suppressing action [X represents a halogen atom, an alkyl group which may be substituted, or the like, Y represents hydrogen atom or an alkyl group which may be substituted, and Z represents hydrogen atom or an alkyl group which may be substituted].
SUBSTITUTED PYRAZINONE DERIVATIVES FOR USE AS A MEDICINE
申请人:Andres-Gil Jose Ignacio
公开号:US20090111801A1
公开(公告)日:2009-04-30
The present invention concerns substituted pyrazinone derivatives according to the general Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim
1
, having selective α
2C
-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.