880468-89-3Relevant articles and documents
Preparation method of lacosamide
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Paragraph 0033-0034, (2020/07/02)
The invention provides a novel methylation method of a lacosamide synthesis intermediate, which comprises the following steps: methylating a compound I in a reaction solvent at a proper temperature byusing trimethyloxyonium tetrafluoroborate as a methylation reagent under alkaline condition to obtain a methylation product II. The reaction formula is shown in the specification. The method has theadvantages of mild reaction condition, simple post-treatment, green methylation reagent, no high toxicity and high reaction yield, and conforms to the safe and environment-friendly green chemical concept. The method is suitable for laboratory small-scale preparation and large-scale industrial production.
AN IMPROVED PROCESS FOR THE PREPARATION OF LACOSAMIDE
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, (2018/04/17)
The present invention relates to an improved process for the synthesis of (R)- Lacosamide in which free base of O-methyl-N-benzyl-D-Serinamide is not isolated before acylation. The process avoids the use of column chromatography and chiral resolution for the preparation of different stages of Lacosamide.
A raco amide intermediate of methylation method (by machine translation)
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Paragraph 0043; 0044; 0046; 0048; 0049, (2017/07/21)
The invention is mainly discloses a synthesis scheme in the process of synthesis of the methylation reaction method, the toxic and carcinogenic, cheap a methylating agent such as methyl benzene sulfonic acid methyl ester and the like as the alkylating agent, using inexpensive alkali such as potassium hydroxide to methylation reaction. The present invention can effectively avoid the generation of the N - methyl impurity, and the productive rate is high, will not produce the racemization, hydroxy has good selectivity, is more suitable for industrial production. (by machine translation)