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A continuous-flow synthesis of aziridines by palladium-catalyzed C(sp3)-H activation is described. The new flow reaction could be combined with an aziridine-ring-opening reaction to give highly functionalized aliphaticamines through a consecutive process. A predictive mechanistic model was developed and used to design the C-H activation flow process and illustrates an approach towards first-principles design based on novel catalytic reactions.