Stable Vicinal Bisketene Equivalents for Aryne Diels-Alder Reactions [0.03%]
稳定的邻近双环乙烷衍生物用于芳炔狄尔斯-阿尔德反应
Jessica E Budwitz,Christopher G Newton
Jessica E Budwitz
2,5-Bis(tert-butyldimethylsilyloxy)thiophenes are introduced as bench-stable Diels-Alder dienes for reaction with arynes as dienophiles. Ring-opening of the cycloadducts can be achieved via TBAF-promoted desilylation, providing convergent r...
Joel M Smith
Joel M Smith
Recent developments in the isotopic labeling of heteroarenes may prove to be useful in the realms of biomedical science, materials chemistry, and fundamental organic chemistry. The use of the age-old Zincke reaction, or tactical variants th...
Efficient Regioselective Synthesis of Benzimidazoles and Azabenzimidazoles to Enable the Rapid Development of Structure-Activity Relationships for Activation of SLACK Potassium Channels [0.03%]
高效区域选择性合成苯并咪唑和氮杂苯并咪唑以快速开发激活SLACK钾通道的结构活性关系
Paul K Peprah,Brittany D Spitznagel,Yu Du et al.
Paul K Peprah et al.
The sodium activated potassium channel known as SLACK (KNa1.1 or Slo2.2) is widely expressed in the central nervous system and represents a potential target for the treatment of several neurological disorders. While much recent progress has...
Cyclic Imine-BF3 Complexes as Precursors for Functionalized Azacycles [0.03%]
用于制备功能化氮杂环的环状环胺-氟硼酸复合物
Kamal Bhatt,Daniel Seidel
Kamal Bhatt
Due to the relative instability and low electrophilicity of enolizable alicyclic imines, their functionalization commonly requires cryogenic temperatures and highly reactive nucleophiles such as organolithium compounds. Stable BF3 adducts o...
Collaboration in Natural Product Total Synthesis: Carolacton - A Decade of Discovery [0.03%]
自然产物全合成中的合作精神——Carolacton的十年研究历程
Amy E Solinski,William M Wuest
Amy E Solinski
Carolacton, a macrocyclic natural product with impressive anti-biofilm biological activity, has been a focus in multiple research groups for the past decade. Chemists and biologists, alike, have been interested in uncovering the mechanism o...
Chen-Yan Cai,Tian Qin
Chen-Yan Cai
Selective C3 functionalization of unbiased pyridines represents a significant challenge in organic synthesis. While seminal work in this area has enabled access to various C3-substituted pyridines via dearomatized intermediates, the direct ...
Tandem Diboration-Protoboration of Terminal Alkynes: A Practical Route to α-Substituted Alkenyl Boronates [0.03%]
末端炔烃的串联亲电硼化-去对甲苯磺酰基硼化反应：制备α-取代烯基硼酸酯的新方法
Ziyin Kong,Jimin Park,Muchun Fei et al.
Ziyin Kong et al.
A practical method is introduced for the catalytic conversion of terminal alkynes into α-substituted vinyl boronic esters. The process employs catalytic amounts of nanoparticle-supported gold catalysts and catalytic amounts of copper to ef...
Regioselective Formation of Pyridines by Cycloaddition/Cycloreversion of 1,4-Oxazinone Precursors with Bisalkyne Substrates [0.03%]
双叠烯底物与1,4-氧氮杂环己酮前体通过环加成/环逆转区域选择性形成吡啶类化合物
Graydon J Andres,Seth E Anderson,Adrianne M Kinsey et al.
Graydon J Andres et al.
This study explores the merged cycloaddition/cycloreversion of a 1,4-oxazinone substrate and conjugated bisalkyne precursors. Good regioselectivity in the Diels-Alder operation is observed and pyridines bearing 3-alkynyl functionality are a...
Aniekan Okon,Anton Morgunov,Jinyi Yang et al.
Aniekan Okon et al.
Bioreversible protein esterification is a simple, customizable, and traceless strategy for the exogenous delivery of proteins into mammalian cells. Enabling this protein delivery strategy are α-aryl-α-diazoamides bearing a tolyl moiety. T...
Inverting the Conventional Site Selectivity of Cross-Coupling of 2,4-Dichloropyrimidines [0.03%]
2,4-二氯嘧啶交叉偶联的非传统位点选择性 inversion 研究
Oliver D Jackson,Sharon R Neufeldt
Oliver D Jackson
Cross-coupling and nucleophilic aromatic substitution reactions of 2,4-dihalopyrimidines generally favor reaction at the C4 site, especially in the absence of other substituents on the pyrimidine ring. Here we review our recent discovery of...