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Herein, we report an efficient strategy for the rapid construction of 1,4-oxazines starting from simple α-amino ketones and diazo pyruvates under mild reaction conditions. This transformation is efficiently catalyzed by RuCl3 through a tandem N-H insertion/cyclization sequence via an enol formation. This reaction shows broad functional group tolerance, and the resulting 1,4-oxazine products show promising anticancer activities toward HCT116.Supportive stromal cells of mesenchymal origins regulate vascular morphogenesis in developmental,