PIFA-Mediated Coupling of Vindoline with β-Ketoesters and Related Model Velbanamine Precursors [0.03%]
PIFA介导的长春地辛与β-酮酸酯及相关范兰胺模型化合物的偶联反应
Jiajun Zhang,Nazanin Haddadpour,Bin Cai et al.
Jiajun Zhang et al.
A study of PIFA-mediated arylations of advanced model β-ketoesters and related substrates with vindoline for the total synthesis of vinblastine and related analogues are reported. The studies demonstrate the viability of the reaction in es...
Kyra L Samony,Justin J Chang,Daniel K Kim
Kyra L Samony
Protecting groups are commonplace in organic synthesis and appear often in the form of dioxanes and dioxolanes. 1,3-Dioxolanes can be used for the protection of both diol and carbonyl motifs. Our group has been increasingly interested in al...
Iron Porphyrin Catalysts Induce Stereospecific Glycosylation with Glycal Epoxides [0.03%]
铁卟啉催化剂可诱导糖醛酸与环氧糖脎的立体选择性糖基化反应
Hao Xu,Dakang Zhang,Xiao-Wen Zhang et al.
Hao Xu et al.
This account highlights an iron porphyrin-catalyzed highly stereospecific glycosylation method for glycal epoxides. This method is effective for a wide variety of previously challenging, hindered secondary sugar acceptors and a broad array ...
TiCl4-Promoted Intramolecular Friedel-Crafts Cyclization of α-Keto-phenylbutanoates: Synthesis of Substituted Indane and Indene Derivatives [0.03%]
四氯化钛促进的α-酮基苯基丁酸酯的分子内傅克环化反应：杂环取代吲哚化合物的合成
Arun K Ghosh,Tristan John McDonald
Arun K Ghosh
We report a TiCl4-mediated intramolecular Friedel-Crafts type cyclization that provides convenient access to functionalized indane and indene derivatives. Reaction of α-ketoester derivatives bearing a phenylethyl side chain with 1.2 equiv ...
Promita Biswas,David C Powers
Promita Biswas
Aziridines are the smallest nitrogen-containing heterocycles and are responsible for the biological activity of aziridine-natural products and active pharmaceutical ingredients (APIs). Classically, aziridines are prepared from acyclic precu...
Unlocking electrophilic N-aryl intermediates from aryl azides, nitroarenes, and aryl amines in cyclization-migration reactions [0.03%]
通过环化迁移反应从芳基叠氮化合物、硝基芳烃和芳胺活化生成亲电子的芳基中间体
Tom G Driver
Tom G Driver
An Account of our development of reactions to construct N-heterocycles by triggering cyclization-migration tandem reactions from aryl azides, nitroarenes, and aryl amines is described. The reactivity patterns of metal N-aryl nitrenes, nitro...
Nucleophilic Additions of Organolithium Reagents to Heterocyclic Aldimines [0.03%]
有机锂试剂对杂环醛亚胺的亲核加成反应
Justin Baek,Walker A Hoisington,Evelyn S Galgano et al.
Justin Baek et al.
The addition of alkyllithium reagents to heterocyclic aldimines is described. This method is a straightforward two-step procedure from the starting aldehyde and amine with one purification. The ability to use unprotected indole carboxaldehy...
Fluorine-Thiol Displacement Stapling on the Disordered αB of pKID Domain Increases Its Helicity and Affinity to KIX [0.03%]
αB无序区的氟代硫醇交换 stapling 增加了pKID域的螺旋性和与KIX的亲和力
Carson B Cohen,Andrew J Andrews,Rongsheng E Wang
Carson B Cohen
The development of high-affinity ligands specifically targeting intrinsically disordered protein interactions has remained challenging due to the lack of well-defined binding pockets and shallow binding surfaces commonly found at their inte...
Zachary E Paikin,Ana Villalobos Galindo,Monika Raj
Zachary E Paikin
Protein macrocyclization is a pivotal process in the stabilization of protein structures, significantly enhancing their proteolytic stability and thermostability. While nature elegantly accomplishes this through a diverse family of ligases,...
Regioselective Aldehyde Decarbonylation through Palladium-Catalyzed Nitrile Boronic Acid Cross-Coupling [0.03%]
通过钯催化腈硼酸交叉偶联实现醛的区域选择性脱碳氧酰基化反应
Zachary E Paikin,John M Talbott,Monika Raj
Zachary E Paikin
Aldehyde decarbonylation is a vital chemical transformation in the synthesis of natural products. Nature accomplishes this process through a family of decarbonylase enzymes, while in the laboratory, harsh transition metals and elevated temp...