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ARCHIMICA

机译:架构

摘要

process for the preparation of lacosamide. A novel process for the synthesis of lacosamide using d, l-serine as a starting material is described, in which the hydroxy methylation reaction is performed using a low cost base such as, and is not a low cost alkylating agent. Toxic and non-carcinogenic, such as methyl ptoluenesulfonate, the r enantiometer is isolated from the racemic mixture of lacosamide after selective hydrolysis of acetamide, salification of the racemic mixture with a chiral acid (hx *) in an organic solvent, decomposition. of the diastereoisomeric mixture, preferably by precipitation of the enantiometer r, and subsequent acetylation of the optically pure intermediate.
机译:拉考酰胺的制备方法。描述了一种以d,1-丝氨酸为起始原料合成拉考酰胺的新颖方法,其中羟甲基化反应是使用低成本的碱而不是低成本的烷基化剂进行的。有毒和非致癌物质,例如对甲苯磺酸甲酯,在对乙酰胺进行选择性水解后,从拉可酰胺的外消旋混合物中分离出对映体,然后在有机溶剂中用手性酸(hx *)将外消旋混合物成盐。非对映异构混合物的制备,优选通过对映异构体r的沉淀,以及随后的光学纯中间体的乙酰化。

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