Palladium-Catalyzed γ-Selective Arylation of Zincated Boc-Allylamines
摘要:
The regio- and diastereoselective arylation of Boc-protected allylamines was performed via a one-pot lithiation/transmetalation to zinc/cross-coupling sequence, through an appropriate choice of a phosphine ligand. A variety of γ-arylated products were obtained in moderate to good yield, and the products could be directly transformed into valuable γ-arylamines and β-aryl aldehydes.
Palladium-Catalyzed γ-Selective Arylation of Zincated Boc-Allylamines
摘要:
The regio- and diastereoselective arylation of Boc-protected allylamines was performed via a one-pot lithiation/transmetalation to zinc/cross-coupling sequence, through an appropriate choice of a phosphine ligand. A variety of γ-arylated products were obtained in moderate to good yield, and the products could be directly transformed into valuable γ-arylamines and β-aryl aldehydes.
[EN] NOVEL 2-PIPERIDIN-1-YL-ACETAMIDE COMPOUNDS FOR USE AS TANKYRASE INHIBITORS<br/>[FR] NOUVEAUX COMPOSÉS 2-PIPERIDIN-1-YL-ACETAMIDE UTILISABLES EN TANT QU'INHIBITEURS DE TANKYRASE
申请人:NOVARTIS AG
公开号:WO2013012723A1
公开(公告)日:2013-01-24
The present invention provides for compounds of formula (I), wherein R1-R5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
Synthesis of 2-Aminoindolizines by 1,3-Dipolar Cycloaddition of Pyridinium Ylides with Electron-Deficient Ynamides
作者:Julien Brioche、Christophe Meyer、Janine Cossy
DOI:10.1021/acs.orglett.5b01205
日期:2015.6.5
possessing an ynoate or an ynone moiety, have been successfully involved for the first time in a 1,3-dipolarcycloaddition with stabilized pyridiniumylides. These reactions afford an efficient and general access toward a variety of substituted 2-aminoindolizines which can serve as useful precursors for the synthesis of other more complex nitrogen heterocycles.
[EN] BIARYL DERIVATIVES AS GPR120 AGONISTS<br/>[FR] DÉRIVÉS DE BIARYLE EN TANT QU'AGONISTES DE GPR120
申请人:LG LIFE SCIENCES LTD
公开号:WO2014209034A1
公开(公告)日:2014-12-31
The present invention relates to biaryl derivatives of Formula 1, a method for preparing the same, a pharmaceutical composition comprising the same and use thereof. The biaryl derivatives of Formula 1 according to the present invention promote GLP-1 formation in the gastrointestinal tract and improve insulin resistance in the liver or in muscle due to anti-inflammatory action in macrophages, lipocytes, etc., and can accordingly be effectively used for preventing or treating diabetes, complications of diabetes, obesity, non-alcoholic fatty liver, steatohepatitis, osteoporosis or inflammation.
The present invention relates to novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ.
本发明涉及新型视黄醇相关孤儿受体γ(RORγ)调节剂及其在治疗由RORγ介导的疾病中的应用。
FXA INHIBITORS WITH CYCLIC AMIDOXIME OR CYCLIC AMIDRAZONE AS P4 SUBUNIT, PROCESSES FOR THEIR PREPARATIONS, AND PHARMACEUTICAL COMPOSITIONS AND DERIVATIVES THEREOF
申请人:Song Ho Young
公开号:US20110112083A1
公开(公告)日:2011-05-12
The present invention relates to novel oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group, pharmaceutically acceptable salts thereof, methods for preparing the same and pharmaceutical compositions comprising the same. The oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group or the pharmaceutically acceptable salts thereof can be effectively used for the treatment of thromboembolism and tumor as an anticoagulant based on the inhibition of factor Xa.