Scheme 2.
Synthetic route of a series of neocryptolepine derivatives. Reagents and conditions: (a) trichloroacetyl chloride, pyridine, KOH, 85% (b) N-chlorosucccinimide, 1,4-dimethylpiperazine, CH2Cl2, 0 °C, 2 h; trichloroacetic acid, RT, 2 h, 64%; (c) diphenyl ether, reflux, 1.3 h; (d) POCl3, toluene, reflux, 6–12 h, 70%; (e) amino derivatives or hydroxyl, DMF; (f) KOH; (g) ethanol, heat.