Two step syntheses of fused quinoxaline-benzodiazepines and bis-benzodiazepines.
A two-step solution phase synthesis employing a double UDC (Ugi/Deprotect/Cyclize) strategy has been utilized to obtain fused 6,7,6,6-quinoxalinone-benzodiazepines and 6,7,7,6-bis-benzodiazepines. Optimization of the methodology to produce these tetracyclic scaffolds was enabled by microwave irradiation, incorporation of trifluoroethanol as solvent, and the use of the convertible isocyanide, 4-tert-butyl cyclohexen-1-yl isocyanide.
Xu
Zhigang
Z
College of Pharmacy, Department of Pharmacology and Toxicology, Division of Medicinal Chemistry, BIO5 Institute, Southwest Comprehensive Center for Drug Discovery and Development, University of Arizona, AZ 85721.
Dietrich
Justin
J
Shaw
Arthur Y
AY
Hulme
Christopher
C