Efficient Resolution of Racemic Guaifenesin via Batch-Preferential Crystallization Processes,Organic Process Research & Development

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Efficient Resolution of Racemic Guaifenesin via Batch-Preferential Crystallization Processes
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2019-12-20 , DOI: 10.1021/acs.oprd.9b00413
Francesca Cascella ₁ , Erik Temmel ₂ , Andreas Seidel-Morgenstern _{1,

2} , Heike Lorenz ₂

Affiliation

The potential of enantioseparation processes based on preferential crystallization (PC) in single and coupled batch configuration is demonstrated for the active pharmaceutical ingredient (API) guaifenesin. After presenting thermodynamics and kinetics for the system guaifenesin in isopropanol, two batch crystallization-based separation approaches are exploited. First, single-batch-preferential crystallization in two different solvents has been studied. The results are described in terms of productivity, purity, and yield, with an emphasis on the role of the solvent in the enantioseparation outcome. Second, we demonstrate the applicability and performance of an alternative approach, namely, coupled batch-preferential crystallization and selective dissolution (CPCD) for the system guaifenesin/isopropanol, and highlight the advantages and drawbacks of this promising concept.

中文翻译：

通过批次优先结晶过程有效拆分外消旋瓜皮菌素

对于活性药物成分（API）愈创甘油醚，证明了在单批次和偶联批次配置中基于优先结晶（PC）的对映体分离工艺的潜力。在介绍了愈创甘油醚在异丙醇中的热力学和动力学后，开发了两种基于分批结晶的分离方法。首先，已经研究了在两种不同溶剂中的单批次优先结晶。用生产率，纯度和产率来描述结果，重点是溶剂在对映体分离结果中的作用。其次，我们证明了另一种方法的适用性和性能，即愈创甘油醚/异丙醇体系的分批优先结晶和选择性溶解（CPCD），

更新日期：2019-12-21

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