Mechanochemistry for “no solvent, no base” preparation of hydantoin-based active pharmaceutical ingredients: nitrofurantoin and dantrolene - Université de Montpellier Accéder directement au contenu
Article Dans Une Revue Green Chemistry Année : 2018

Mechanochemistry for “no solvent, no base” preparation of hydantoin-based active pharmaceutical ingredients: nitrofurantoin and dantrolene

Résumé

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.

Dates et versions

hal-01845433 , version 1 (20-07-2018)

Identifiants

Citer

Evelina Colacino, Andrea Porcheddu, Ivan Halasz, Clarence Charnay, Francesco Delogu, et al.. Mechanochemistry for “no solvent, no base” preparation of hydantoin-based active pharmaceutical ingredients: nitrofurantoin and dantrolene. Green Chemistry, 2018, 20 (13), pp.2973 - 2977. ⟨10.1039/c8gc01345d⟩. ⟨hal-01845433⟩
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