Efficient Cu-catalyzed Atom Transfer Radical Addition Reactions of Fluoroalkylsulfonyl Chlorides with Electron-deficient Alkenes Induced by Visible Light
作者:Xiao-Jun Tang、William R. Dolbier
DOI:10.1002/anie.201412199
日期:2015.3.27
Fluoroalkylsulfonyl chlorides, RfSO2Cl, in which Rf=CF3, C4F9, CF2H, CH2F, and CH2CF3, are used as a source of fluorinated radicals to add fluoroalkyl groups to electron‐deficient, unsaturated carbonyl compounds. Photochemical conditions, using Cu mediation, are used to produce the respective α‐chloro‐β‐fluoroalkylcarbonyl products in excellent yields through an atom transferradicaladdition (ATRA) process
氟烷基磺酰氯,R f SO 2 Cl,其中R f= CF 3,C 4 F 9,CF 2 H,CH 2 F和CH 2 CF 3,被用作氟自由基的来源以向电子中添加氟烷基。不足的不饱和羰基化合物。通过铜介导的光化学条件,可通过原子转移自由基加成(ATRA)工艺以优异的产率生产相应的α-氯-β-氟代烷基羰基产物。α-氯取代基的容易亲核取代会导致产物进一步多样化的功能。
[EN] HETEROCYCLIC COMPOUND AND USE THEREOF<br/>[FR] COMPOSÉ HÉTÉROCYCLIQUE ET SON UTILISATION
申请人:TAKEDA PHARMACEUTICALS CO
公开号:WO2019027058A1
公开(公告)日:2019-02-07
The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I) : wherein each symbol is as described in the specification, or a salt thereof, is useful as an agent for the prophylaxis treatment of narcolepsy.
[EN] TDO2 AND IDO1 INHIBITORS<br/>[FR] INHIBITEURS DE TDO2 ET IDO1
申请人:GENENTECH INC
公开号:WO2019005559A1
公开(公告)日:2019-01-03
Presently provided are inhibitors of cellularly expressed TD02 and IDO1, and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2,3 dioxygenase and indoleamine 2,3-dioxygenase 1; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.
[EN] MEDIUM- OR MACRO-CYCLIC BENZYL-SUBSTITUTED HETEROCYCLE DERIVATIVES AND THEIR USES AS OREXIN-2 RECEPTOR AGONISTS<br/>[FR] DÉRIVÉS HÉTÉROCYCLIQUES SUBSTITUÉS PAR UN BENZYLE MOYEN CYCLE OU MACROCYCLIQUE ET LEURS UTILISATIONS EN TANT QU'AGONISTES DU RÉCEPTEUR DE L'OREXINE 2
申请人:OREXIA THERAPEUTICS LTD
公开号:WO2022051583A1
公开(公告)日:2022-03-10
The present disclosure relates to compounds of Formula (I') and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for modulating orexin-2 receptor activity and may be used m the treatment of disorders in which orexin-2 receptor activity is implicated, such as narcolepsy, a hypersomnia disorder, a neurodegenerative disorder, a symptom of a rare genetic disorder, a mental health disorder, a metabolic syndrome, osteoporosis, cardiac failure, coma, or facilitating emergence from anaesthesia.