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The coupling reaction allows simple structural fragments to be constructed and sequentially assembled by C-X bond to synthesize a variety of active molecular frameworks. Different from the traditional single-metal catalyst, the synergistic effect of bimetal provides special catalytic activity that cannot be obtained by traditional single-metal catalyst, thus emerging as an efficient alternative mode. In this paper, we used CuAl bimetallic heterogeneous mesoporous materials to participate in the sequential assembly of CS and CN bonds, which effectively catalyzed the synthesis of 2-substituted benzothiazole heterocyclic systems. In addition, GW610 with antitumor activity was synthesized easily and efficiently by this strategy.