Search engine for discovering works of Art, research articles, and books related to Art and Culture
Javascript must be enabled to continue!
Synthesis of α- and β-Carbolines by a Metalation/Negishi Cross-Coupling/SNAr Reaction Sequence
View through CrossRef
Carbolines are privileged scaffolds in medicinal chemistry, and therefore, novel and efficient approaches to their synthesis are in high demand. An efficient method for the synthesis of α- and β-carbolines from fluoropyridines and 2-haloanilines is reported. This streamlined procedure consists of a four-step directed ortho-lithiation, zincation, Negishi cross-coupling, and intramolecular nucleophilic aromatic substitution, providing access to a diverse set of functionalised carbolines. While the procedure is applicable to batch conditions, the generation of arylzinc intermediates in continuous flow has been demonstrated .
Title: Synthesis of α- and β-Carbolines by a Metalation/Negishi Cross-Coupling/SNAr Reaction Sequence
Description:
Carbolines are privileged scaffolds in medicinal chemistry, and therefore, novel and efficient approaches to their synthesis are in high demand.
An efficient method for the synthesis of α- and β-carbolines from fluoropyridines and 2-haloanilines is reported.
This streamlined procedure consists of a four-step directed ortho-lithiation, zincation, Negishi cross-coupling, and intramolecular nucleophilic aromatic substitution, providing access to a diverse set of functionalised carbolines.
While the procedure is applicable to batch conditions, the generation of arylzinc intermediates in continuous flow has been demonstrated .
Related Results
Isolation, characterization and semi-synthesis of natural products dimeric amide alkaloids
Isolation, characterization and semi-synthesis of natural products dimeric amide alkaloids
Isolation, characterization of natural products dimeric amide alkaloids from roots of the Piper chaba Hunter. The synthesis of these products using intermolecular [4+2] cycloaddit...
Synthesis of α- and β-Carbolines by a Metalation/Negishi Cross-Coupling/SNAr Reaction Sequence
Synthesis of α- and β-Carbolines by a Metalation/Negishi Cross-Coupling/SNAr Reaction Sequence
Carbolines are considered to be privileged scaffolds in medicinal chemistry. An efficient method for the synthesis of α- and β-carbolines from fluoropyridines and 2-haloanilines is...
Heteroatom‐Facilitated Lithiations
Heteroatom‐Facilitated Lithiations
Abstract
Some 25 years have elapsed since the topic of metalation reactions was reviewed by Gilman and Morton. The intervening years have been notable for in...
The interaction between neural populations: Additive versus diffusive coupling
The interaction between neural populations: Additive versus diffusive coupling
Abstract
Models of networks of populations of neurons commonly assume that the interactions between neural populations are via
...
a-Aryl-a-Heteroarylmalononitriles via Proton-Transfer Dual-Ionization Nucleophilic Aromatic Substitution
a-Aryl-a-Heteroarylmalononitriles via Proton-Transfer Dual-Ionization Nucleophilic Aromatic Substitution
Herein we report the synthesis of a-aryl-a-heteroarylmalononitriles. Retrosynthetically, such molecules should be readily available from a-arylmalononitrile and haloheterocycles vi...
Synthesis of Benzofuropyridines and Dibenzofurans by a Metalation/Negishi Cross-Coupling/SNAr Reaction Sequence
Synthesis of Benzofuropyridines and Dibenzofurans by a Metalation/Negishi Cross-Coupling/SNAr Reaction Sequence
An efficient methodology for the synthesis of benzofuropyridines and dibenzofurans from fluoropyridines or fluoroarenes and 2-bromophenyl acetates is reported. This streamlined one...
Influence of Different Coupling Modes on the Robustness of Smart Grid under Targeted Attack
Influence of Different Coupling Modes on the Robustness of Smart Grid under Targeted Attack
Many previous works only focused on the cascading failure of global coupling of one-to-one structures in interdependent networks, but the local coupling of dual coupling structures...
Metalation and activation of Zn2+ enzymes via early secretory pathway-resident ZNT proteins
Metalation and activation of Zn2+ enzymes via early secretory pathway-resident ZNT proteins
Zinc (Zn2+), an essential trace element, binds to various proteins, including enzymes, transcription factors, channels, and signaling molecules and their receptors, to regulate the...