One-step synthesis of carbocycles substituted with amines from simple starting materials remains rare. We recently developed intermolecular [3+2] annulation of cyclopropylanilines with alkenes and alkynes that enable this one-step synthesis. Herein, we report our findings for a fullscale study of the annulation. Significant expansion of the substrate scope for both cyclopropylanilines and alkynes is achieved. A range of structurally diverse carbocycles substituted with amines is prepared.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4478291 | PMC |
| http://dx.doi.org/10.1002/adsc.201400742 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Hydrophilic Ethylene Glycol Fragments: A Determinant Affecting the Therapeutic Index of Paclitaxel Prodrug Nanoassemblies.
ACS Cent Sci
December 2024
Department of Pharmaceutics, Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang, 110016, China.
Prodrug-based nanoassemblies are promising platforms for cancer therapy. Prodrugs typically consist of three main components: drug modules, intelligent response modules, and modification modules. However, the available modification modules are usually hydrophobic aliphatic side chains, which affect the activation efficiency of the prodrugs.
View Article and Find Full Text PDFPiperine as a molecular bridge mediates a ternary coamorphous system of polyphenols with enhanced pharmaceutical properties.
Int J Pharm
December 2024
School of Pharmaceutical Sciences, Nanjing Tech University, Nanjing 211816, China. Electronic address:
The coamorphous formulations have attracted increasing interest due to enhanced solubility and bioavailability, together with synergistic pharmacological effects. In this study, a ternary coamorphous system of polyphenols was successfully prepared, wherein baicalein (Bai) and resveratrol (Res) were constructed into a single-phase coamorphous system mediated by piperine (Pip). FTIR and ss C NMR spectra together with quantum chemical calculation and molecular dynamics simulation suggested Pip as a molecular bridge connected Bai and Res molecules through π-π stacking and hydrogen bonding interactions.
View Article and Find Full Text PDFStudy on the formation mechanism and effective manipulation of polymorphs and solvates in Osimertinib-Caffeic acid multi-component crystal with distinct properties.
Int J Pharm
December 2024
Guangdong Provincial Key Lab of Green Chemical Product Technology, School of Chemistry and Chemical Engineering, South China University of Technology, Guangzhou 510640, China. Electronic address:
Investigating the formation mechanism and effective manipulation of multi-component crystal polymorphs is crucial for facilitating industrial drug development. Herein, five novel Osimertinib-caffeic acid forms were first strategically tailored by varying solvent selection. Theoretical analysis demonstrated this polymorphism is correlated with multiple hydrogen bond donors-acceptors within multi-component system, which provides manipulation space for reconfiguration of intermolecular interactions and structural competition, while solvent further induced or involved in hydrogen-bonded rearrangements.
View Article and Find Full Text PDFUnderstanding the mechanism of saccharides type and concentration affecting texture of freeze-dried pectin-CMC cryogels through experiment and molecular dynamic simulation.
Int J Biol Macromol
December 2024
Institute of Food Science and Technology, Chinese Academy of Agricultural Sciences (CAAS), Key Laboratory of Agro-Products Processing, Ministry of Agriculture and Rural Affairs, Beijing, China. Electronic address:
Saccharides are the dominant factor shaping the texture of freeze-dried products. This study investigated the impact of various molecular-weight saccharides at different concentrations on the physical properties and intermolecular interactions of pectin-CMC cryogels by experiment and molecular dynamic (MD) simulations. Results showed that the increased shrinkage of cryogels and enhanced molecular interactions between saccharides and pectin-CMC were mechanisms that enhanced the hardness of cryogels.
View Article and Find Full Text PDFMicroencapsulation of Pickering nanoemulsions containing walnut oil stabilized using soy protein-curcumin composite nanoparticles: Fabrication and evaluation of a novel plant-based milk substitute.
Food Chem
December 2024
School of Food and Biological Engineering, Key Laboratory of Modern Agricultural Products Processing of Anhui Province, Hefei University of Technology, Hefei 230601, China. Electronic address:
Plant protein-stabilized Pickering nanoemulsions show potential as plant-based milk substitutes; however, their stability is challenged by mechanical stress during transportation and oxidative deterioration during storage. Herein, soybean isolate protein-curcumin composite nanoparticle (SPI-Cur-NPs)-stabilized Pickering nanoemulsions were converted into microcapsule powders via spray-drying with maltodextrin (MD), trehalose anhydrous (TA), and inulin (IN) as wall materials. Robust intermolecular hydrogen bonds and an amorphous structure were formed using composite wall materials, reducing microcapsule surface fissures while improving encapsulation rate (92.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!