[EN] 2,4-DIAMINO-6,7-DIHYDRO-5H-PYRROLO[2,3]PYRIMIDINE DERIVATIVES AS FAK/Pyk2 INHIBITORS<br/>[FR] DÉRIVÉS DE 2,4-DIAMINO-6,7-DIHYDRO-5H-PYRROLO[2,3]PYRIMIDINE COMME INHIBITEURS DE FAK/PYK2
申请人:CENTAURUS BIOPHARMA CO LTD
公开号:WO2012092880A1
公开(公告)日:2012-07-12
The invention relates to a novel class of 2,4-diamino-6,7-dihydro-5H-pyrrolo[2,3]pyrimidine derivatives as a FAK and/or Pyk2 inhibitor, to a process for their preparation, and to a composition thereof, as well as to use of the compounds for the inhibiting FAK and/or Pyk2 and method for the treatment of a FAK and/ or Pyk2 mediated disorder or disease.
Iron-Catalyzed Hydroamination and Hydroetherification of Unactivated Alkenes
作者:Paul T. Marcyk、Silas P. Cook
DOI:10.1021/acs.orglett.9b00427
日期:2019.3.1
The hydrofunctionalization of alkenes, explored for over 100 years, offers the potential for a direct, atom-economical approach to value-added products. While thermodynamically favored, the kinetic barrier to such processes necessitates the use of catalysts to control selectivity and reactivity. Modern variants typically rely on noble metals that require different ligands for each class of hydrofunctionalization
selective aromatic deuteriation of various sulfonylureas and tertiary sulfonamides, as well as for a broad range of secondary sulfonamides. Based on a comprehensive screening of readily available Ir catalysts, the Kerr-type NHC catalyst 5 proved to be most efficient in the HIE reaction of secondary sulfonamides and sulfonylureas. However, for tertiary sulfonamides, the commercially available Burgess catalyst
我们首次报告了各种磺酰脲类和叔磺酰胺以及各种仲磺酰胺的选择性芳烃氘化的优化氢同位素交换 (HIE) 条件。基于对容易获得的 Ir 催化剂的全面筛选,证明 Kerr 型 NHC 催化剂 5 在仲磺酰胺和磺脲类的 HIE 反应中最有效。然而,对于叔磺酰胺,尚未用于 HIE 反应的市售 Burgess 催化剂 6 导致氘的掺入量高得多。最后,我们测试了用于标记一系列磺胺药物的新 HIE 协议,并调整了条件以允许选择性氚标记。
Functionalization of Mesoporous Carbon with Superbasic MgO Nanoparticles for the Efficient Synthesis of Sulfinamides
highly crystalline small‐size cubic‐phase MgOnanoparticles with a high dispersion. The basicity of the MgO‐supported mesoporouscarbons can also be controlled by simply changing the loading of the MgO and the pore diameter of the support. These materials have been employed as heterogeneous catalysts for the first time in the selective synthesis of sulfinamides. Among the catalysts investigated, the support
Nickel-Catalyzed Denitrogenative Cyclization of 1,2,3,4-Benzothiatriazin-1,1(2<i>H</i>)-dioxides with Arynes To Synthesize Biaryl Sultams
作者:Vijaykumar H. Thorat、Yu-Lin Tsai、Yong-Ran Huang、Chien-Hong Cheng、Jen-Chieh Hsieh
DOI:10.1021/acs.orglett.2c00920
日期:2022.4.22
Herein, we report the nickel-catalyzed denitrogenative cyclization reaction of 1,2,3,4-benzothiatriazine-1,1-dioxides with arynes to generate the polysubstituted biaryl sultams with tolerance of a wide diversity of substituents on every subunit. The mechanistic study indicates that the reaction is initiated by the formation of a diradical species, which reacts with a nickel complex to form a nickelacycle