Continuous-flow microreactor multi-step synthesis of an aminonaphthalene derivative as starting material for the preparation of novel anticancer agents

A multi-step synthesis of the aminonaphthalene derivate 1 as a key intermediate in the synthesis of the duocarmycin based prodrug 2 for a selective treatment of cancer in a microreactor is described. The conditions for the synthesis in the batch mode were adjusted for application in a microreactor and the results of both methods were compared showing that the transformations in the microreactor in most cases give similar or even better results with the advantage of a continuous-flow production, higher safety and faster reactions with an empirical accelerating factor of F = 3–10.