Scheme 2.
Solid-phase synthesis of 3,4-disubstituted dihydroquinazolin-2(1H)-ones (CA1–CA5). (a) Rink resin was swollen in DMF, 24 h; Fmoc-X-OH, HOBt, DIC, 3 h; (b) Scaffold, HOBt, DIC, 8 h; (c) NH2-R2, DIEA, 20 h; (d) Pd(PPh3)4, PhSiH3, DCM, 50 min (2×); (e) CDI, pyridine, DCM, 12 h; (f) 2 M SnCl2·2H2O/DMF, 24 h (2×); (g) R3-COOH, HATU, DIEA, DMAP, overnight; R3SO2Cl, DIEA, DCM, overnight; (h) TFA cocktail, 3 h.
