Related Experiment Video
Updated: Feb 15, 2026
11:27
Synthesis and Characterization of Functionalized Metal-organic Frameworks
Published on: September 5, 2014
49.3K
Domino Carbopalladation/C-H Activation as a Quick Access to Polycyclic Frameworks
Nemai Saha1,2, Haiwen Wang1, Shengyi Zhang1
1State Key Laboratory of Oncology in South China, Collaborative Innovation Center for Cancer Medicine, Sun Yat-sen University Cancer Center , 651 Dongfeng East Road, Guangzhou 510060, China.
Organic Letters
|January 11, 2018
Summary
A novel domino reaction synthesizes bioactive heterocycles like oxindole and isoquinoline using palladium catalysis. This method creates unique polycyclic frameworks valuable for drug discovery applications.
Area of Science:
- Organic Chemistry
- Medicinal Chemistry
- Synthetic Chemistry
Background:
- Heterocyclic compounds are crucial scaffolds in medicinal chemistry.
- Developing efficient synthetic routes to complex heterocycles is an ongoing challenge.
Purpose of the Study:
- To present a new domino reaction for synthesizing fused bioactive heterocycles.
- To explore the utility of palladium-catalyzed sequential carbopalladation/C-H activation.
Main Methods:
- Utilized N-alkenyl iodobiaryls as substrates.
- Employed a common palladium catalyst to initiate the domino reaction.
- Investigated sequential carbopalladation and C-H activation steps.
Main Results:
- Successfully synthesized novel polycyclic frameworks.
- Demonstrated the formation of heterocycles incorporating oxindole, indoline, and isoquinoline cores.
- Established a new domino reaction pathway.
Conclusions:
- The developed domino reaction offers an efficient route to complex heterocyclic structures.
- The synthesized frameworks are potential sources for fragment-based drug discovery.
- Palladium-catalyzed sequential carbopalladation/C-H activation is a powerful strategy for constructing polycyclic systems.
Related Concept Videos
02:42Eukaryotic Transcription Activators
12.9K
Transcription activators are proteins that promote the transcription of genes from DNA to RNA. In most cases, these proteins contain two separate domains ‒ a domain that binds to DNA and a domain for activating transcription; however, in some cases, a single domain is responsible for both binding and activation of transcription, as seen in the glucocorticoid receptor and MyoD.
The binding domains are capable of recognizing and interacting with regulatory sequences on the DNA. These...
The binding domains are capable of recognizing and interacting with regulatory sequences on the DNA. These...
12.9K
02:04Co-activators and Co-repressors
8.7K
Gene transcription is regulated by the synergistic action of several proteins that form a complex at a gene regulatory site. This is observed in eukaryotes, where the regulation of gene expression is a complex process. Regulatory proteins in eukaryotes can broadly be classified into two types – regulators that bind directly to specific DNA sequences and co-regulators that associate with regulatory proteins but cannot directly bind to the DNA. These co-regulators are further divided into...
8.7K
02:26tRNA Activation
23.2K
Aminoacyl-tRNA synthetases are present in both eukaryotes and bacteria. Though eukaryotes have 20 different aminoacyl-tRNA synthetases to couple to 20 amino acids, many bacteria do not have genes for all of these aminoacyl-tRNA synthetases. Despite this, they still use all 20 amino acids to synthesize their proteins. For instance, some bacteria do not have the gene encoding the enzyme that couples glutamine with its partner tRNA. In these organisms, one enzyme adds glutamic acid to all of the...
23.2K
01:26Activation Energy
87.2K
Activation energy is the minimum amount of energy necessary for a chemical reaction to move forward. The higher the activation energy, the slower the rate of the reaction. However, adding heat to the reaction will increase the rate, since it causes molecules to move faster and increase the likelihood that molecules will collide. The collision and breaking of bonds represents the uphill phase of a reaction and generates the transition state. The transition state is an unstable high-energy state...
87.2K
01:55Secondary Active Transport
138.4K
One example of how cells use the energy contained in electrochemical gradients is demonstrated by glucose transport into cells. The ion vital to this process is sodium (Na+), which is typically present in higher concentrations extracellularly than in the cytosol. Such a concentration difference is due, in part, to the action of an enzyme “pump” embedded in the cellular membrane that actively expels Na+ from a cell. Importantly, as this pump contributes to the high concentration of...
138.4K
01:47Primary Active Transport
201.2K
In contrast to passive transport, active transport involves a substance being moved through membranes in a direction against its concentration or electrochemical gradient. There are two types of active transport: primary active transport and secondary active transport. Primary active transport utilizes chemical energy from ATP to drive protein pumps that are embedded in the cell membrane. With energy from ATP, the pumps transport ions against their electrochemical gradients—a direction...
201.2K