First functionalization by metallation of the benzene moiety of quinazolines. Diazines XIX.

Article abstract of DOI:10.1016/S0040-4020(97)00046-X

The first lithiation on the benzene moiety of 4-substituted quinazolines has been highlighted. According to the nature and position of various directing groups, an exceptional regioselective metallation occured at position C₈, peri to the N-1 ring nitrogen. This method allows an easy access to a large range of new substituted quinazolines.