Ramesh Garlapati, Narender Pottabathini, Venkateshwarlu Gurram
Sep 19, 2012
Citations
0
Influential Citations
9
Citations
Journal
Tetrahedron Letters
Abstract
Abstract 6-Halo-2-cyclopropyl-3-(pyridyl-3-ylmethyl) quinazolin-4(3H)-one derivatives have been synthesized and utilized for amination reactions with aryl, heteroaryl and alkyl amines. Optimization of reaction conditions with different catalysts, ligands, bases, and solvents was conducted. The combination of Pd2(dba)3 with DavePhos (L3) proved to be best for these conversions in the presence of NaOtBu in 1,4-dioxane at 100 °C. The relative reactivities of 6-bromo and 6-chloro-2,3-disubstitued quinazolinones with p-toluidine were conducted and as anticipated the 6-bromo analogue was totally consumed and 6-chloro derivative was completely unreactive.