Preparation method of sodium ion channel blocker CNV1014802 hydrochloride form

The invention relates to the field of pharmaceutical chemicals, in particular to a novel preparation method of sodium ion channel blocker (GSK1014802) CNV1014802 hydrochloride for inhibiting sodium ion internal flow, which is a high-selectivity asymmetric synthesis method, aldehyde and a chiral indu...

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Hauptverfasser: CHAI BAOHONG, WEN ZHAOFENG, KAI YONGPING, LU GANG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to the field of pharmaceutical chemicals, in particular to a novel preparation method of sodium ion channel blocker (GSK1014802) CNV1014802 hydrochloride for inhibiting sodium ion internal flow, which is a high-selectivity asymmetric synthesis method, aldehyde and a chiral induction reagent are subjected to dehydration condensation to generate Schiff base, then the Schiff base and a lithium reagent and the like are subjected to an addition reaction, and the high-selectivity chiral intermediate is obtained. Then reactions such as ring closing and step-by-step oxidation are performed to obtain the target compound. Compared with the existing reported synthesis method, the method has the advantages that the process cost can be reduced, the safety is better, and the chiral purity of the compound is higher. 本发明涉及医药化工领域,具体来说,涉及一种用来抑制钠离子内流的钠离子通道阻滞剂(GSK1014802)CNV1014802盐酸盐的新制备方法,其是一种高选择性的不对称合成方法,通过醛与手性诱导试剂脱水缩合生成席夫碱,然后与锂试剂等进行加成反应,得到高选择性的手性中间体。再通过关环、分步氧化等反应,即可得到目标化合物。较现有报导的合成方法相比,可以实现降低工艺成本、安全性更好、