Non-Kekulé Bi-Blatter Diradicals: Phenyl versus Electron-Deficient Heteroaromatic Linkers [0.03%]
非凯库勒双层 diradical：苯基与电子贫乏的杂芳基连接体
Tiankun Guo,Li Zhang,Xiaoyu Wang et al.
Tiankun Guo et al.
A series of stable non-Kekulé 1,2,4-benzotriazinyl-based diradicals bridged by phenyl (1), pyridine (2), pyrazine (3), and pyrimidine (4) groups have been successfully isolated. Combined experimental and theoretical analyses confirm that a...
Unlocking C-N Bond Formation via a Two-Photon ETU-FRET Relay with Near-Infrared Light [0.03%]
利用近红外光的两光子ETU-FRET中继解锁C-N键形成反应
Yue Zeng,Yukai Yao,Yuchen Zhu et al.
Yue Zeng et al.
The first two-photon upconversion photocatalysis for challenging C-N bond formations was reported. A robust, recyclable NaYF4,Yb:Er/Co3O4/g-C3N4 nanosheet platform operated under mild, aerobic conditions with near-infrared light via an ETU-...
AbClick Pro H: Scavenger-Free, Traceless Lys248 Conjugation Via O-Acyl Hydroxamate Chemistry for Homogeneous Antibody-Drug Conjugates (ADCs) [0.03%]
用于均相抗体药物偶联物的无清除剂、无痕迹Lys248连接子-H：通过O酰基羟胺化学实现
Jinyoung Son,Jin Woo Seo,Sun Hee Park et al.
Jinyoung Son et al.
A traceless O-acyl hydroxamate Fc-binding peptide linker enables rapid, scavenger-free, and site-selective conjugation at Lys248 of human IgG1. The resulting homogeneous DAR2 antibody-drug conjugates (ADCs) retain antigen binding and intern...
Enantioselective Synthesis of Functionalized 2,2-Disubstituted Piperidines Enabled by Pd-Catalyzed Decarboxylative Asymmetric Allylic Alkylation [0.03%]
钯催化脱羧不对称烯丙基烷基化反应合成功能化2，2-双取代的哌啶化合物
Zhenzhen Wang,Dan Chen,Junhai Chang et al.
Zhenzhen Wang et al.
Herein, we report a palladium-catalyzed decarboxylative asymmetric allylic alkylation (Pd-DAAA) for the synthesis of enantioenriched 2,2-disubstituted piperidines. This method efficiently constructs aza-quaternary stereocenters with high en...
Mallory-Type Reactivity of 1,2-Dihydroazaborinines: 6π-Electrocyclization-[1,5]-H Shift Cascade toward BN-Doped Polycyclic Frameworks [0.03%]
1,2-二氢氮杂硼叶环类化合物的马勒里型反应性：通过6π电环化-[1,5]氢迁移级联反应形成含BN的杂多环骨架
Sonja M Biebl,Robert C Richter,Markus Ströbele et al.
Sonja M Biebl et al.
1,2-Dihydro-1,2-azaborinines exhibit highly selective substitution-dependent photochemistry, yielding either Dewar or benzvalene isomers. Through targeted substitution, an o-BN-terphenyl framework is constructed, which undergoes 6π-electro...
Copper-Catalyzed Trifunctionalization of Alkynes: One-Pot Assembly of Antifungal Benzofuro[3,2- d]pyrimidine-Containing Fused Heterocycles [0.03%]
铜催化炔烃三官能化反应：一锅法制备含抗真菌并苯并呋喃并[3,2-d]嘧啶的稠环杂环化合物
Zhi-Jie Kang,Ben-Jun Han,Yuan-Qi Li et al.
Zhi-Jie Kang et al.
A copper-catalyzed, three-component tandem reaction for the synthesis of benzofuro[3,2-d]pyrimidine-containing fused heterocycles has been developed. This one-pot protocol efficiently couples terminal alkynes, salicylaldehydes, and α-amino...
B(C6F5)3-Catalyzed (5 + 1)-Annulation of Enynamides with Trihydrosilanes en Route to the Synthesis of 1,4-Azasilines [0.03%]
硼催化剂催化内炔酰胺与三硅烷的（5+1）环化反应合成1,4-氮杂硅素化合物
Yu Fan,Jun Jing,Xuan Li et al.
Yu Fan et al.
Silaazacycles are emerging as promising heavier bioisosteres of N-heterocycles in drug discovery. Among them, 1,4-azasiline, a versatile scaffold that enables access to diverse silaazacycles, has remained underexplored, largely due to the l...
Peilin Tian,Jing Xu,Rongbiao Tong
Peilin Tian
Withanolide D is a highly oxygenated steroid with a broad spectrum of biological activities (potent antitumor properties) and thus has stimulated considerable interest from synthetic chemists. Herein, we describe a concise 10-step synthesis...
Access to Alkylative/Hydrodefluorination of Trifluoromethyl Ketones Using Photoexcited Dihydropyridines [0.03%]
光激发二氢吡啶催化的三氟甲基酮的烯丙基化/脱氟氢化反应
Surajit Das,Debasis Maity,Biprajit Paul et al.
Surajit Das et al.
A convenient strategy for selective and challenging single C-F bond functionalization of trifluoromethyl ketones has been introduced under visible light irradiation. Photoexcited 1,4-DHP serves a dual purpose as a reductant and a source of ...
Enantioselective Cobalt-Catalyzed C-H Activation and Annulation of Indole-3-carboxamides with Alkynes: Access to Axially Chiral γ-Carbolinones [0.03%]
手性钴催化吲哚-3-甲酰胺与炔烃的C-H活化环化反应合成轴手性γ-色满酮类化合物
Qi-Liang Yang,Chun Gao,Dong-Chao Wang et al.
Qi-Liang Yang et al.
A Co(II)/Salox-catalyzed atroposelective C-H activation/annulation of indole-3-carboxamides with either internal or terminal alkynes was developed that provides facile access to a broad range of γ-carbolinone derivatives having C-N axial, ...