Enantioselective Photoredox Catalysis Enabled by Proton-Coupled Electron Transfer: Development of an Asymmetric Aza-Pinacol Cyclization
作者:Lydia J. Rono、Hatice G. Yayla、David Y. Wang、Michael F. Armstrong、Robert R. Knowles
DOI:10.1021/ja4100595
日期:2013.11.27
protocol for the reductive coupling of ketones and hydrazones is reported. These reactions proceed through neutral ketyl radical intermediates generated via a concerted proton-coupled electron transfer (PCET) event jointly mediated by a chiral phosphoric acid catalyst and the photoredox catalyst Ir(ppy)2(dtbpy)PF6. Remarkably, these neutral ketyl radicals appear to remain H-bonded to the chiral conjugate
报道了第一个用于酮和腙还原偶联的高度对映选择性催化方案。这些反应通过由手性磷酸催化剂和光氧化还原催化剂 Ir(ppy)2(dtbpy)PF6 共同介导的协同质子耦合电子转移 (PCET) 事件产生的中性羰基自由基中间体进行。值得注意的是,在随后的 CC 键形成步骤过程中,这些中性羰基自由基似乎保持与布朗斯台德酸的手性共轭碱 H 键合,从而提供具有优异水平的非对映选择性和对映选择性的顺式 1,2-氨基醇衍生物. 这项工作首次证明了不对称催化中协同 PCET 活化的可行性和潜在益处。
[EN] CYCLOALKYL NITRILE PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS<br/>[FR] CYCLOALKYLNITRILE PYRAZOLOPYRIDONES UTILISÉES COMME INHIBITEURS DE LA JANUS KINASE
申请人:MERCK SHARP & DOHME
公开号:WO2014146490A1
公开(公告)日:2014-09-25
Compounds of formula I are provided, which are JAK inhibitors and are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
GPR119 agonist compounds of the formula:
and pharmaceutical compositions for the treatment of diabetes and obesity.
GPR119激动剂化合物的公式:
以及用于治疗糖尿病和肥胖的药物组合物。
[EN] 4-AMINO-5-OXO-7, 8-DIHYDROPYRIMIDO [5,4-F] [1,4] OXAZEPIN-6 (5H) -YL) PHENYL DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF<br/>[FR] DÉRIVÉS DE 4-AMINO-5-OXO-7,8-DIHYDROPYRIMIDO[5,4-F][1,4]OXAZÉPIN-6(5H)-YL)PHÉNYLE
申请人:PFIZER
公开号:WO2010086820A1
公开(公告)日:2010-08-05
The invention provides compounds of Formula (I), wherein R1, R2a, R2b, R3, m and A are as defined herein, as well as compositions thereof and methods for treating a disease, condition or disorder that is modulated by the inhibition of the diacylglycerol O-acyltransferase 1 (DGAT-1) enzyme by administering the compounds of the present invention and/or compositions thereof.
The invention provides compounds of the general Formula (I)
where R
1
, R
2
, and A are defined herein, as well as the preparation, compositions and uses thereof.