High-Throughput Classical Chiral Resolution Screening of Synthetic Intermediates: Effects of Resolving Agents, Crystallization Solvents, and Other Factors,Organic Process Research & Development

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High-Throughput Classical Chiral Resolution Screening of Synthetic Intermediates: Effects of Resolving Agents, Crystallization Solvents, and Other Factors
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2020-08-20 , DOI: 10.1021/acs.oprd.0c00348
Jun Qiu ₁ , Jason M. Stevens ₁

Affiliation

Using a statistical Z-score methodology, enantiomeric excess (ee) data from our historical high-throughput classical chiral resolution screens were analyzed. In total, 19 of the screens used chiral acids as resolving agents, and 20 used chiral bases. The results show clear trends in terms of the selection of chiral acids/bases in conjunction with a crystallization solvent. We rank ordered resolving agents, solvents, and resolving agent/solvent combinations by applying the Z-score method on the ee of isolated solids, and provided recommendations on executing more efficient classical chiral resolution screening for synthetic intermediates.

中文翻译：

合成中间体的高通量经典手性拆分筛查：拆分试剂，结晶溶剂和其他因素的影响

使用统计的Z评分方法，分析了来自我们历史悠久的高通量经典手性拆分屏幕的对映体过量（ee）数据。总共有19个筛选使用手性酸作为拆分剂，还有20个使用手性碱。结果表明与结晶溶剂一起在选择手性酸/碱方面有明显的趋势。通过在分离的固体ee上应用Z评分法，我们对有序的拆分剂，溶剂和拆分剂/溶剂组合进行了排名，并提供了对合成中间体进行更有效的经典手性拆分筛查的建议。

更新日期：2020-09-20

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