The syntheses of several key intermediates were carried out as outlined in Scheme When R 1 substituents were pyridyls or the rest of the aryl groups, an alternative route as Scheme 3 depicts was employed. After mono-substitution of 4-bromo-2,6difluorobenzaldehyde with bis(2,4-dimethoxybenzyl)amine, the quinazoline skeleton was constructed by a similar method to that of 25. Then, a Suzuki reaction between the obtained 31 and the boronic acid pinacol ester 23 occurred, followed by Buchwald coupling reactions with various aryl or heteroaryl halides to furnish 33a-33k.