Issue 4, 2019

Flow-oriented synthetic design in the continuous preparation of the aryl piperazine drug flibanserin

Abstract

An uninterrupted, four-step continuous-flow sequence was developed for the preparation of the aryl piperazine-type serotonin receptor modulator drug, flibanserin. The unprecedented route was designed for efficient operation in flow, consisting of heterogeneously catalyzed reductive amination reactions, benzimidazolone formation using the protecting group as a building block, and biphasic flow deprotection integrated with in-line purification. Gas–liquid and liquid–liquid separations facilitate the coupling of the reaction steps and aid removal of excess reagents, which make the system capable of steady-state operation without manual interaction.

Graphical abstract: Flow-oriented synthetic design in the continuous preparation of the aryl piperazine drug flibanserin

Supplementary files

Article information

Article type
Communication
Submitted
19 Oct 2018
Accepted
20 Dec 2018
First published
07 Jan 2019

React. Chem. Eng., 2019,4, 652-657

Flow-oriented synthetic design in the continuous preparation of the aryl piperazine drug flibanserin

P. Bana, Á. Szigetvári, J. Kóti, J. Éles and I. Greiner, React. Chem. Eng., 2019, 4, 652 DOI: 10.1039/C8RE00266E

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