1253790-58-7Relevant articles and documents
Improved Synthesis and Impurity Identification of (R)-Lacosamide
Yang, Anjiang,Hu, Feifei,Li, Zhong,Chen, Mengdi,Cai, Jianguang,Wang, Linghui,Zhang, Tao,Zhao, Chuanmeng,Zhang, Fuli
, p. 818 - 824 (2019/04/01)
An improved synthesis of Lacosamide 1 with high purity has been developed. Critical parameters of each step were identified as well as the impurities generated. Moreover, a creative method to improve chiral purity and stability of the key intermediate (R)-2-amino-N-benzyl-3-methoxypropionamide 10 by forming salt with an achiral acid (phosphoric acid) was discovered to ensure the chiral purity of (R)-Lacosamide. Phosphoric acid was further developed for the deprotection of the Boc group.
Improved preparation method of modified lacosamide
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Paragraph 0036; 0041-0043, (2017/08/31)
The invention discloses an improved preparation method of modified lacosamide, which is simple to operate, high in chiral purity and low in cost. According to the improved preparation method, in step 1, amidation is carried out on amino by utilizing di-tert butyl dicarbonate (Boc for short), wherein conditions are moderate and the chiral purity is high and at least reaches 90 percent or more; in step 4, high-selectivity dimethyl sulfate is used as a methylation reagent; the cost is low and the conditions are moderate; the methylation yield is high and the improved preparation method is more suitable for large-scale application. The improved preparation method has the most important innovation points that the Boc is used as an N-protection agent and a Boc protecting group can be simply and conveniently removed by adding acid and a hydrogenation removal means does not need to be used. Secondly, the low-price dimethyl sulfate is used for carrying out methylation and the conditions are moderate; the methylation yield is high and the improved preparation method is more suitable for large-scale application.
A raco amide analogs and its preparation method
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Paragraph 0098; 0099; 0100; 0101, (2017/08/25)
The invention discloses a Lacosamide analogue and a preparation method thereof, and provides the Lacosamide analogue shown in a formula (I). The invention further provides the preparation method of the Lacosamide analogue shown in the formula (I), including: subjecting a compound shown in a formula (II) and methylated solution in two-phase solvent of organic solvent and water, and in the presence of alkali and phase transfer catalyst to substitution reaction for 20 to 100 hours, so as to obtain the compound shown in the formula (I). The Lacosamide analogue shown in the formula (I) is a necessity for quality control of Lacosamide; the preparation method can be used for efficiently synthesizing the analogue.