New (E)‐3‐(2‐aminoquinoxalin‐3‐yl)‐1‐arylprop‐2‐en‐1‐ones are prepared through the multi‐component reaction of 3‐substituted‐2‐chloroqunoxalines, calcium carbide, and aromatic aldehydes in the presence of diethylamine, catalyzed by Pd/Cu in acetonitrile. This synthetic strategy presents an acetylene molecule linking the quinoxaline scaffold to an aldehyde moiety for construction of quinoxaline chalcone by two carbon‐carbon bond coupling reactions. This one‐pot process provides an efficient and direct method for the synthesis of new quinoxaline chalcones from the low‐cost calcium carbide with good yields. A number of synthesized compounds were screened for their in vitro anti‐bacterial activity against Gram‐positive and Gram‐negative bacteria using a well‐diffusion method.

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4-(2-Substituted-[1,3]thiazolo[3,2-a]benzimidazol-3-yl)quinazolin-2-amines were prepared by the reaction of 2,4-dichloroquinazoline, terminal alkynes, secondary amines, and 1H-benzo[d]imidazole-2(3H)-thione in the presence of palladium catalyst.

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