Development of a Scalable Route to a Pyrrolidone Compound via a Hydroxyfuranone,Organic Process Research & Development

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Development of a Scalable Route to a Pyrrolidone Compound via a Hydroxyfuranone
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2022-03-15 , DOI: 10.1021/acs.oprd.1c00350
Lorene Calvano ₁ , Frédéric Gilson ₁ , Frank Driessens ₁ , Sylvain Petit ₁

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Herein, we describe the preparation of pyrrolidone compound 1 as a potential antiepileptic drug. The key steps of this synthetic route are based on the preparation of a heterocyclic amine and its condensation with a hydroxyfuranone in a three-step one-pot process. The development of the synthesis led to decreased route complexity and removal of chromatographic purifications. These improvements were demonstrated at scale by the production of 700 g of this pyrrolidone.

中文翻译：

通过羟基呋喃酮开发吡咯烷酮化合物的可扩展路线

在此，我们将吡咯烷酮化合物1的制备描述为一种潜在的抗癫痫药物。该合成路线的关键步骤是基于杂环胺的制备及其与羟基呋喃酮在三步一锅法中的缩合反应。合成的发展导致路线复杂性的降低和色谱纯化的去除。这些改进通过生产 700 克这种吡咯烷酮得到大规模证明。

更新日期：2022-03-15

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