Mohammed K Abd El-Gaber,Mario Djugovski,Tzu-Yu Huang et al.
Mohammed K Abd El-Gaber et al.
Incorporating fluorine into azoles is not only a common practice but also an essential tactic in medicinal chemistry, due to their ability to fine-tune a molecule's physicochemical, pharmacokinetic, and pharmacodynamic profiles. The strateg...
Total Synthesis of Tabernanthine and Ibogaline: Rapid Access to Nosyl Tryptamines [0.03%]
长春花生物碱盐酸塔巴宁因和伊博加因的全合成：Nosyl-氯乙基衍生物高效制备苦杏仁酸缩氨酶类生物碱的新策略
Alexander J Hughes,Steven D Townsend
Alexander J Hughes
We describe the first total syntheses of tabernanthine and ibogaline. Entry to these iboga alkaloid natural products is enabled by a thermal coupling of indoles and aziridines to furnish the requisite nosyl tryptamine starting materials. Th...
Disrupting Substance Use Disorder: The Chemistry of Iboga Alkaloids [0.03%]
_IBOGA 碱对人体物质使用障碍的干预作用及其化学机理分析_
Alexander J Hughes,Charles R Hamelink,Steven D Townsend
Alexander J Hughes
The iboga alkaloids are a family of monoterpene indole alkaloids first discovered from the root of Tabernanthe iboga. The major alkaloid constituent in the root, ibogaine, has garnered interest for its anti-addictive properties. Ibogaine ha...
Elucidating Fluorine Steering Effects in Diels-Alder Reactions Interfaced with Charge-Enhanced Reactivity [0.03%]
揭示介电负增强反应活性的狄尔斯-阿尔德反应中的氟导向效应
Sabrina Hoford,Julius Jan,Jeffrey N Johnston et al.
Sabrina Hoford et al.
Fluorinated molecules are core to contemporary drug discovery programs and critical for advancing innovation in numerous fields. In merging these important chemical themes, fluorinated Diels-Alder cycloaddition products are a particularly a...
Lukas S Vogl,Matthias Bechmann,Mario Waser
Lukas S Vogl
Isothioureas (ITUs) represent a powerful family of (chiral) Lewis base organocatalysts. Interestingly, the Brønsted basicity of these frequently used compounds has so far not systematically been investigated. Thus, we have now determined t...
Exploring Interrupted Nazarov Cyclizations Using Tethered Sulfonamide Nucleophiles: Insights into Capture Pathways [0.03%]
带有连接磺酰胺亲核试剂的Nazarov环化中断的研究：捕获途径的见解
Aleksa Milosavljevic,Jackson J Hernandez,Patrycia K Zybura et al.
Aleksa Milosavljevic et al.
This manuscript describes a study of diverse reaction outcomes that stem from the ionization of aza-alkynyl-Prins adducts. Experimental results have demonstrated unexpected behavior in the nitrogen-containing systems compared to the analogo...
Fun With Unusual Functional Groups: Sulfamates, Phosphoramidates, and Di-tert-butyl Silanols [0.03%]
奇特官能团的有趣之处：硫代氨基甲酸酯、磷酰胺和双叔丁氧基硅烷
Shyam Sathyamoorthi
Shyam Sathyamoorthi
Compared to ubiquitous functional groups such as alcohols, carboxylic acids, amines, and amides, which serve as central "actors" in most organic reactions, sulfamates, phosphoramidates, and di-tert-butyl silanols have historically been view...
n-Bu4NI/K2S2O8-MEDIATED C-N COUPLING BETWEEN ALDEHYDES AND AMIDES [0.03%]
醛和酰胺的C-N偶联反应生成酮亚胺和希杰酸酯的新方法
Xiaochen Liu,Samual Hee,Netanel G Sapir et al.
Xiaochen Liu et al.
n-Bu4NI/K2S2O8 mediated C-N coupling between aldehydes and amides is reported. A strong electronic effect is observed on the aromatic aldehyde substrates. The transformylation from aldehyde to amide takes place exclusively when an aromatic ...
Chiral Lewis Base-Catalysed Asymmetric Syntheses of Benzo-fused ϵ-Lactones [0.03%]
手性质子催化剂催化的苯并环ε-内酯的不对称合成
Lotte Stockhammer,Maximilian Radetzky,Syeda Sadia Khatoon et al.
Lotte Stockhammer et al.
We herein report a two-step protocol for the asymmetric synthesis of novel chiral benzofused ϵ-lactones starting from O-protected hydroxymethyl-para-quinone methides and activated aryl esters. By using chiral isothiourea Lewis base catalys...
Cooperative Chiral Lewis Base/Palladium-Catalyzed Asymmetric Syntheses of Methylene-Containing δ-Lactams [0.03%]
手性Lewis碱/钯协同催化含亚甲基δ-内酰胺的不对称合成
Paul Zebrowski,Uwe Monkowius,Mario Waser
Paul Zebrowski
We herein report a two-step approach for the enantioselective synthesis of novel chiral δ-lactams. By using a cooperative chiral ITU/achiral Pd-catalyst system, this protocol proceeds via an asymmetric α-allylation of activated aryl ester...