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  • 1 Laboratoires Fournier S.A., an Abbott company, Chemical, Design and Synthesis Unit, 50 rue de Dijon, 21310, Daix, France
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Abstract

A series of substituted indole-2-carboxylic acid ethyl esters and aza-indole analogs have been prepared using continuous-flow hydrogenation. The identification of some key parameters using a design of experiments (DoE)-based approach allowed efficient optimization of each synthesis. The scale-up study for the multigram preparation of one model indole substrate showed the importance of working at steady state with the H-Cube pparatus. A new useful method for the easy preparation of substituted indoles in various quantities is presented.

Supplementary Materials

    • Supplementary Material