A5076080431- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Axial and Atropisomeric Chirality Synthesis
- Neurotransmitter Receptor Influence on Behavior
- Molecular spectroscopy and chirality
- Receptor Mechanisms and Signaling
- Alkaloids: synthesis and pharmacology
- Chemical synthesis and alkaloids
- Catalytic C–H Functionalization Methods
- Synthesis and Biological Evaluation
- Synthesis of Indole Derivatives
- Ubiquitin and proteasome pathways
- Plant and Fungal Species Descriptions
- Protein Degradation and Inhibitors
- HER2/EGFR in Cancer Research
- Pharmacological Receptor Mechanisms and Effects
Zhejiang University
2021-2024
Wenzhou University
2023
Shanghai Institute of Pharmaceutical Industry
2019
China Pharmaceutical University
2019
We report herein an unprecedented atroposelective dynamic kinetic resolution of Bringmann's lactones with C-nucleophiles. By the use activated isocyanides as reagent, a wide range novel axially chiral oxazole-substituted biaryl phenols were accessed in high yields enantioselectivities. Key to success this process lies tandem addition lactone substrate followed by rapid cyclization, overcoming challenge stereochemical leakage induced lactol formation.
Herein, we report an unprecedented strategy for the simultaneous construction of a remote C–N stereogenic axis and three contiguous carbon centers via silver-catalyzed desymmetrizative [3 + 2] cycloaddition prochiral N-aryl maleimides with activated isocyanides. This method features operational simplicity, wide substrate scope, high efficiency, good to excellent stereoselectivity. Notably, it represents first example catalytic enantioselective synthesis atropisomers use
The catalytic reaction of biaryl lactams with activated isocyanides is reported for the first time. By employing a cooperative system, oxazole-containing axially chiral anilines were obtained in high yields excellent enantioselectivities. key to success lies atroposelective amide C-N bond cleavage isocyanides.
Here, an Ir/Zn-cocatalyzed atroposelective [2+2+2] cycloaddition of 1,6-diynes and ynamines was developed, forging various functionalized C─N axially chiral indoles pyrroles in generally good to excellent yields (up 99%), chemoselectivities, high enantioselectivities 98% enantiomeric excess) with wide substrate scope. This cocatalyzed strategy not only provided alternative promising reliable way for asymmetric alkyne cyclotrimerization easy handle but also settled the issues previous...
Elevated expression levels and enhanced activity of androgen receptor (AR) proteins are key factors in the development androgenetic alopecia (AGA). AR proteolysis-targeting chimera (PROTAC) degraders have shown therapeutic potential, but their poor skin permeability requires invasive delivery methods. In this study, we conducted a structure feature analysis to investigate effects different linkers E3 ligands PROTACs on retention properties degradation potency. Among these, compound C6 was...