Enzymatic C42 Diversification of Rapamycin Identifies a Potent Butyryl-Modified Anticancer Derivative [0.03%]
酶促C42多样化研究雷帕霉素以获得一种有效的丁酰化抗肿瘤衍生物
Yining Liu,Hengyu Li,Jinyue Pu et al.
Yining Liu et al.
A highly regioselective, one-step lipase-catalyzed method enabled the diversification of rapamycin at its C42 position, producing 10 derivatives (4 novel). Biological screening identified derivative 9 as a potent lead compound with superior...
Palladium-Catalyzed Synthesis of 2-Sulfenyl Benzofused Heterocycles through Domino Cyclization/Thiolation of gem-Dibromoolefins [0.03%]
gem-二溴 olefins的串联环化/硫醇化反应钯催化合成苯并稠合杂环化合物中的2-硫基enzofused heterocycles的合成通过gem-二溴OLEFINS的串联环化/硫醇化反应 Palladium催化
Shuaichen Zheng,Shaowen Ling,Yingxian Wu et al.
Shuaichen Zheng et al.
Herein, we describe a straightforward, thiol-free palladium-catalyzed umpolung protocol that uses mild conditions to stitch together readily available dibromoolefins and disulfides, yielding a diverse array of 2-sulfenyl benzofused heterocy...
Purine-Based Fused Tetracyclic Energetic Materials with Balanced Energetic Performance [0.03%]
具有平衡性能的嘌呤基融合四环型发射药类材料
Sagar Nehe,Rishabh Gupta,Vikas D Ghule et al.
Sagar Nehe et al.
A series of purine-based fused tetracyclic energetic materials was synthesized. Incorporation of explosophoric groups afforded compounds with high densities (1.82-1.85 g cm-3), high positive heats of formation (433.6-709.0 kJ mol-1), and go...
Visible-Light-Driven Modular Synthesis of Isoquinolinone Derivatives via Palladium-Catalyzed Radical 6-endo Annulation of Aryl Halides [0.03%]
钯催化自由基环加成反应合成异喹啉酮类化合物
Fu-Ao Liu,Hongnian Liang,Shuaichen Zheng et al.
Fu-Ao Liu et al.
Herein, a photoexcited-state palladium-catalyzed 6-endo selective annulation reaction of aryl-halide-tethered enamides has been developed, allowing various isoquinolinone motifs synthesized under mild conditions. This approach features oper...
Synthesizing C8-Chiral Substituted 5,6,7,8-Tetrahydroquinolines via Palladium-Catalyzed Enantioselective Arylation of Unactivated C(sp3)-H Bonds [0.03%]
钯催化未活化C(sp3)‒H键的对映选择性芳基化合成C8-手性的5,6,7,8-四氢异喹啉类化合物
Zhi-Jing Guo,Jun-Feng Wang,Yu-Xuan Teng et al.
Zhi-Jing Guo et al.
Herein, we present a relatively green method for constructing C8-chiral substituted 5,6,7,8-tetrahydroquinoline (THQs) derivatives via palladium-catalyzed enantioselective arylation of unactivated C(sp3)-H bonds, using (S)-2-((tert-butoxyca...
Yubo Zhao,Zhaohui Zong,Qiang Wang et al.
Yubo Zhao et al.
A new carbaporphyrin dimer (8) featuring a π-extended polycyclic aromatic hydrocarbon (PAH) bridge, namely, tetrabenz[a,c,h,j]anthracene (TBA), was synthesized and characterized. Single-crystal X-ray structure analysis revealed that 8 exhi...
Diastereoselective Cyclopropanation with Secondary Diazoacetamides to Access endo-Azabicyclo[3.1.0]hexane-6-carboxamides [0.03%]
次氮基二乙酸酰胺参与的非对映选择性环丙烷化反应合成endo-氮杂双环[3.1.0]己烷-6-羧酸amide类化合物
Terrence-Thang H Nguyen,Takeru Saito,Warren Chang et al.
Terrence-Thang H Nguyen et al.
A dirhodium(II) tetracarboxylate-catalyzed reaction of secondary diazoacetamides with N-Boc-2,5-dihydro-1H-pyrrole results in a highly diastereoselective cyclopropanation for the synthesis of endo-azabicyclo[3.1.0]hexane-6-carboxamides. The...
Visible-Light-Induced Radical Cascade [4 + 2]/[4 + 2] Cycloaddition of Underexplored N-Acryloyl Indoles To Access Dihydropyrido[1,2- a]-indolones [0.03%]
可见光促进的N-丙烯酰基吲哚未探索区域阴离子自由基级联加成反应合成二氢吡啶并[1,2-a]吲哚酮化合物
Cody Bishir,Samuel Milton,Abbey Hubbard et al.
Cody Bishir et al.
We report a visible-light-mediated radical cascade [4 + 2]/[4 + 2] cycloaddition of simple N-acryloyl indoles and N-hydroxyphthalimide esters, which provides a streamlined route to structurally complex dihydropyrido[1,2-a]-indolones. The re...
Metastable Intermediates (Isoindenes, Isofluorenes, and Isobenzofurans) from Alkyne Precursors via Free Carbenes [0.03%]
通过自由卡宾由炔烃前体形成中间体（异吲哚，异荧光素和异苯并呋喃）
Jackson C Orr,Thomas R Hoye
Jackson C Orr
We report here reactions between a free carbene center and a suitably appended π-bond (C═X) that give rise to reactive intermediates that, in turn, undergo various types of additional transformations (cycloadditions, rearrangements, and r...
Synthesis of α-Trifluoromethylated Amines via Fluoroalkylation and Defluoroamination of Indoles [0.03%]
吲哚的含氟化和去氟胺化合成α-三氟甲基胺类化合物
Jinyuan Gao,Man Liu,Meina Li et al.
Jinyuan Gao et al.
We report a novel approach for the sequential perfluoroalkylation and defluoroamination of indoles. This transformation proceeds under mild conditions and exhibits good functional group tolerance, affording a series of valuable α-perfluoro...