Design and Synthesis of Novel Hybrid Molecules against Malaria

Scheme 1

Synthesis of the primaquine-chloroquine hybrid molecules (ratio 1 : 1 [57] and ratio 1 : 2) with an authentic linkage part of primaquine (1). Reagents and conditions: (a) 4,7-dichloroquinoline (0.5 equivalents), neat, 120°C; (b) 4,7-dichloroquinoline (3 equivalents), neat, 120°C.