Scheme 3.
Solid-phase synthesis of 3,4-disubstituted dihydroquinazolin-2(1H)-ones (CA6–CA7). (a) Rink resin was swollen in DMF, 24 h; Scaffold, HOBt, DIC, 8 h; (b) CH3NH2·HCl, K2CO3, DIEA, 20 h; (c) Pd(PPh3)4, PhSiH3, DCM, 50 min (2×); CDI, pyridine, DCM, 12 h; (d) 2 M SnCl2·2H2O/DMF, 24 h (2×); (e) € R3-COOH, HATU, DIEA, DMAP, overnight; R3SO2Cl, DIEA, DCM, overnight; (f) TFA cocktail, 3 h.
