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Abstract <p>A one-pot multicomponent reaction strategy was employed to synthesize 3-methyl-4-arylmethylene-isoxazole-5(4<i>H</i>)-ones from the aromatic/heteroaromatic aldehyde, 1,2-diketone, and hydroxylamine hydrochloride using the hot melt extrusion technique. The use of an extruder eliminates the need for solvents and catalysts, enabling a continuous, scalable, and environmentally friendly process. The protocol has promising features such as shorter reaction times, minimum waste, easy workup and scale-up procedures, broad substrate scope, and moderate to excellent yields. Also, the methodology demonstrates exceptional sustainability, with an E-factor of 0.05, an Eco scale score of 94, and a Process mass intensity of 1.63, thereby showcasing a greener and energy-efficient methodology.</p>

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Hot Melt Extrusion Assisted Synthesis of 3-Methyl-4-arylmethyleneisoxazole-5(4H)-ones: A Continuous and Sustainable Approach

  • 期刊论文

  • 发表日期：

    2025年7月1日

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  • K. S. More,
  • P. D. Nikam,
  • Y. U. Gadkari

摘要

Abstract

A one-pot multicomponent reaction strategy was employed to synthesize 3-methyl-4-arylmethylene-isoxazole-5(4H)-ones from the aromatic/heteroaromatic aldehyde, 1,2-diketone, and hydroxylamine hydrochloride using the hot melt extrusion technique. The use of an extruder eliminates the need for solvents and catalysts, enabling a continuous, scalable, and environmentally friendly process. The protocol has promising features such as shorter reaction times, minimum waste, easy workup and scale-up procedures, broad substrate scope, and moderate to excellent yields. Also, the methodology demonstrates exceptional sustainability, with an E-factor of 0.05, an Eco scale score of 94, and a Process mass intensity of 1.63, thereby showcasing a greener and energy-efficient methodology.