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METHOD OF PREPARING HIGH CHIRAL PURITY LACTAM INTERMEDIATE AND BRIVARACETAM

机译:制备高手性纯度内酰胺中间体和Brivaracetam的方法

摘要

The invention discloses a method of preparing a high chiral purity lactam intermediate and brivaracetam. The invention provides a method of preparing a lactam intermediate compound represented by molecular formula D, the method comprising a step of reducing a compound C to a lactam intermediate D in a solvent by hydrogenation reduction using a heavy metal catalyst and a chiral inducer. Brivaracetam can be prepared with a single step using the lactam intermediate compound represented by molecular formula D of the present invention. The synthesis route is short, reaction conditions are mild, post-treatment is simple, reaction yield is high, chiral selectivity is good, and production cost is low. The conversion rate of the compound C in the reaction is 81%, and the DE value of the compound D is more than 99.0%, which is suitable for industrial production.
机译:本发明公开了一种制备高手性纯度内酰胺中间体和Brivaracetam的方法。 本发明提供了制备由分子式D表示的内酰胺中间体化合物的方法,该方法包括通过使用重金属催化剂和手性诱导剂的氢化还原将化合物C在溶剂中将化合物C还原到内酰胺中间体D的步骤。 Brivaracetam可以使用本发明的分子式D表示的内酰胺中间体化合物用单一步骤制备。 合成途径短,反应条件温和,后处理简单,反应产率高,手性选择性好,生产成本低。 化合物C在反应中的转化率为81%,化合物D的值为99.0%,适用于工业生产。

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