Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 17, Issue 52, Pages 15039-15044Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201102468
Keywords
homogeneous catalysis; isocyanides; insertion; nitrogen heterocycles; palladium; synthetic methods
Categories
Funding
- Netherlands Organization for Scientific Research (NWO)
- Hercules Foundation
Ask authors/readers for more resources
Compared with the widespread use of carbonylative Pd-catalyzed cross-coupling reactions, similar reactions involving isocyanide insertion are almost virgin territory. We investigated the intramolecular imidoylative cross-coupling of N-(2-bromoaryl)amidines, leading to 4-aminoquinazolines. After thorough optimization of the reaction with respect to palladium source and loading, ligand, base, temperature, and solvent, a small library of 4-aminoquinazolines was prepared to determine the scope of this method. Various substituents are tolerated on the amidine and the isocyanide, providing efficient access to a broad range of diversely substituted 4-aminoquinazolines of significant pharmaceutical interest.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available