Overcoming a solid solution system on chiral resolution: combining crystallization and enantioselective dissolution
Overcoming a solid solution system on chiral resolution: combining crystallization and enantioselective dissolution
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克服手性拆分的固溶体体系：结合结晶和对映选择性溶解
DOI：
10.1039/d3cc01352a
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发表时间：
2023
影响因子：
4.9
通讯作者：
Hisaki Ichiro
中科院分区：
文献类型：
--
作者：
Oketani Ryusei;Shiohara Koki;Hisaki Ichiro
采用结晶和对映选择性溶解相结合的方法，成功地拆分了奥扎莫德的关键中间体外消旋-4-氰基-1-氨基茚满，ee值高达96%，并通过二元相图和三元等温线表征了其与二对甲苯酰酒石酸的非对映体盐.然后采用对映选择性溶解来进一步富集对映体。
Chiral resolution of rac-4-cyano-1-aminoindane, a key intermediate of ozanimod, was successfully achieved through a combination of crystallization and enantioselective dissolution with up to 96% ee. The disastereomeric salt with di-p-toluoyl-L-tartaric acid was characterized by the construction of a binary phase diagram and ternary isotherm. Enantioselective dissolution was then employed to further enrich the enantiomer.