Skip to main content
. 2021 Mar 12;12(4):610–616. doi: 10.1021/acsmedchemlett.1c00004

Table 3. Third Series of Quinazoline Derivativesa.

graphic file with name ml1c00004_0009.jpg

entry reagent 1: RNH2 product (yield %) reagent 2: R2B(OH)2 product (yield %)
1 4-methylaniline 8a (53.4) thiophene-2-boronic acid pinacol ester 9a (77.0)
2 3,4-difluorobenzylamine 8b (93.2) 9b (85.3)
a

Reagents and conditions: (a) Corresponding aniline or benzylamine, DMAP, Et3N, toluene, reflux, 3 h; (b) thiophene-2-boronic acid pinacol ester, K2CO3, PdCl2(PPh3)2, toluene/dioxane/water (10:5:8, v/v/v), 90 °C, overnight.