作者:Michael H. Becker、Peter Chua、Robert Downham、Christopher J. Douglas、Neil K. Garg、Sheldon Hiebert、Stefan Jaroch、Richard T. Matsuoka、Joy A. Middleton、Fay W. Ng、Larry E. Overman
DOI:10.1021/ja074300t
日期:2007.10.1
studies toward the complex marine alkaloid sarain A. Various strategies were conceived, setbacks encountered, and solutions developed, ultimately leading to a successful enantioselective totalsynthesis. Our route to (+)-sarain A features a number of key steps, including an asymmetric Michael addition to install the C4'-C3'-C7' stereotriad, an enoxysilane-N-sulfonyliminium ion cyclization to set the C3 quaternary
本文描述了我们对复杂海洋生物碱 sarain A 的合成研究的细节。设想了各种策略、遇到的挫折和开发的解决方案,最终导致对映选择性全合成的成功。我们的 (+)-sarain A 路线具有许多关键步骤,包括不对称迈克尔加成以安装 C4'-C3'-C7' 立体三联体,烯氧基硅烷-N-磺酰亚胺离子环化以设置 C3 季碳立体中心,并组装二氮杂三环十一烷核心、构建13元环的闭环复分解、形成不饱和14元大环的分子内Stille偶联以及叔胺-醛邻近相互作用的后期安装。
[EN] CYCLOHEXYL ACID TRIAZOLE AZOLES AS LPA ANTAGONISTS<br/>[FR] AZOLES TRIAZOLES D'ACIDE CYCLOHEXYLE UTILISÉS EN TANT QU'ANTAGONISTES DE LPA
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2019126094A1
公开(公告)日:2019-06-27
The present invention provides compounds of Formula (I): Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.
[EN] NEW 1-(4-PYRIMIDINYL)-1H-PYRROLO[3,2-c]PYRIDINE DERIVATIVES AS NIK INHIBITORS<br/>[FR] NOUVEAUX DÉRIVÉS DE 1-(4-PYRIMIDINYL)-1H-PYRROLO[3,2-C]PYRIDINE À TITRE D'INHIBITEURS DE NIK
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2015044267A1
公开(公告)日:2015-04-02
The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-κB-inducing kinase (NIK -also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
Synthesis of bicyclo[3.2.2]nonadienones via enantioselective cyclopropanation of racemic cyclohexen-3-yl diazoacetate
作者:Paul Müller、Gérald Bernardinelli、Patrice Nury
DOI:10.1016/s0957-4166(02)00105-2
日期:2002.4
Optically active (1S,5R)-(+)-3-azabicyclo[3.2.2]non-6-en-2-one (+)-7 was synthesized via enantioselective intramolecular cyclopropanation of racemic cyclohexen-3-yl diazoacetate 10 in the presence of [Rh2((2S)-meox}4] catalyst. The cyclopropanation product (−)-9 was converted to the azide 8, which underwent successive Curtius and 3-aza-Cope rearrangements to afford 18, which was reduced to the bicyclic
Compounds of Formula (I) and (II) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.
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