The present disclosure is directed to inhibitors of FASN. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of FASN. For instance, the disclosure is concerned with compounds and compositions for inhibition of FASN, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of FASN, and methods of synthesis of these compounds.
A Redox-Active Supramolecular Fe<sub>4</sub>L<sub>6</sub> Cage Based on Organic Vertices with Acid–Base-Dependent Charge Tunability for Dehydrogenation Catalysis
作者:Yu-Lin Lu、Jia-Qi Song、Yu-Han Qin、Jing Guo、Yin-Hui Huang、Xiao-Dong Zhang、Mei Pan、Cheng-Yong Su
DOI:10.1021/jacs.2c02692
日期:2022.5.18
imidazole proton donor–acceptor motifs and four redox-active Fe centers in an octahedral coordination nanospace. Different from regular supramolecular cages assembled with coordination metal vertices, MOC-63 comprises six ditopic organic-clip ligands as vertices and four tris-chelating Fe(N∩N)3 moieties as faces, thus improving its acid, base, and redox robustness by virtue of cage-stabilized dynamics in
超分子笼化学具有持久的意义,因为作为天然酶的人工蓝图,自组装笼结构不仅提供了底物承载的仿生环境,而且可以在受限的纳米空间中整合活性位点以实现功能协同。在此,我们展示了一种顶点定向的有机夹螯合组装策略,以构建金属-有机笼 Fe 4 L 6 8+ (MOC-63),在八面体中包含 12 个咪唑质子供体 - 受体基序和四个氧化还原活性 Fe 中心协调纳米空间。与常规的以配位金属顶点组装的超分子笼不同,MOC-63 包含六个双位有机夹配体作为顶点和四个三螯合 Fe(N∩N) 3部分作为面,从而通过溶液中的笼稳定动力学提高其酸、碱和氧化还原稳定性。MOC-63 改进了 1,2,3,4-四氢喹啉衍生物的脱氢催化,这是由于超分子笼效应可协同多个 Fe 中心和自由基物种,以加速笼受限纳米空间中多步反应的中间转化。酸碱缓冲咪唑基序在调节总电荷状态以抵抗 pH 变化和调节不同溶剂之间的溶解度方面发挥着至关
Chemoselective One-Pot Synthesis of Functionalized Amino-azaheterocycles Enabled by COware
作者:Thomas A. Clohessy、Alastair Roberts、Eric S. Manas、Vipulkumar K. Patel、Niall A. Anderson、Allan J. B. Watson
DOI:10.1021/acs.orglett.7b03214
日期:2017.12.1
Functionalized bicyclic amino-azaheterocycles are rapidly accessed in a one-pot cross-coupling/reduction sequence enabled by the use of COware. Incompatible reagents are physically separated in a single reaction vessel to effect two chemoselective transformations—Suzuki–Miyaura cross-coupling and heteroarene reduction. The developed method allows access to novel heterocyclic templates, including semisaturated
Photoredox Mediated Acceptorless Dehydrogenative Coupling of Saturated <i>N</i>-Heterocycles
作者:Zongbin Jia、Qi Yang、Long Zhang、Sanzhong Luo
DOI:10.1021/acscatal.9b00123
日期:2019.4.5
We report herein a direct unsymmetric coupling and controllable aromatization reaction of saturatedN-heterocycles enabled by synergistic photoredox and acid catalysis. The reaction furnishes C2–C3 connected biheterocycles in a highly chemo- and regioselective manner under rather mild conditions. Mechanistic studies indicated that the reaction proceeded via enamine-iminium coupling leading to exclusively