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Mechanochemistry for “no solvent, no base” preparation of Hydantoin-based Active Pharmaceutical Ingredients: Nitrofurantoin and Dantrolene.

Abstract

The eco-compatible, base- and waste-free, energy-efficient, low-environmental-impact, gram-scale, mechanochemical preparation of marketed drugs such as Nitrofurantoin (Furantin©), Dantrolene (Dantrium©) and their structurally related derivatives, is herein reported. Not a drop of organic solvent was used for the entire process and high yields of pure compounds were obtained without post-reaction work-up. Hydrazones were stable in the presence of water and gaseous HCl, formed as by-products during the synthesis. Comparative mechanochemical experiments were performed using diverse milling devices and jar materials, the Active Pharmaceutical Ingredients were analyzed by PXRD and green metrics are calculated.

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Supplementary files

Publication details

The article was received on 29 Apr 2018, accepted on 07 Jun 2018 and first published on 08 Jun 2018


Article type: Communication
DOI: 10.1039/C8GC01345D
Citation: Green Chem., 2018, Accepted Manuscript
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    Mechanochemistry for “no solvent, no base” preparation of Hydantoin-based Active Pharmaceutical Ingredients: Nitrofurantoin and Dantrolene.

    E. Colacino, A. Porcheddu, I. Halasz, C. Charnay, F. Delogu, R. Guerra and J. Fullenwarth, Green Chem., 2018, Accepted Manuscript , DOI: 10.1039/C8GC01345D

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