126862-01-9Relevant academic research and scientific papers
Synthetic route of lacosamide
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, (2021/03/31)
The invention discloses a new synthesis route of lacosamide. The new synthesis route comprises the following steps: taking glycine ethyl ester hydrochloride as an initial raw material to react with methylbenzene, benzophenone and p-toluenesulfonic acid to obtain a compound of formula M1; reacting the compound of formula M1 with Xmethyl methyl ether to generate a compound of formula M2; reacting the compound of formula M2 with benzylamine under the catalytic action of sodium ethoxide to generate a compound of formula M3; reacting the compound of formula M3 under the action of acid to generate acompound of formula M4; reacting the compound of formula M4 with Ltartaric acid to generate a compound of formula M5; and enabling the compound of formula M5 to react with acetic anhydride to generate the lacosamide compound. The synthesis route has the advantages that the atom economy is high, the use of isopropyl chloroformate highly toxic products for preparing amide is avoided, the use of methylation reagents methyl iodide or dimethyl sulfate is avoided, the yield is high, and the like.
UNUSUAL N-ACYLATION OF GLYCINE SCHIFF BASES. A SIMPLE APPROACH TO 3,3-DIPHENYLAZIRIDINE-2-CARBOXYLATES
Rao, M. Narayana,Holkar, A. G.,Ayyangar, N. R.
, p. 4717 - 4720 (2007/10/02)
Treatment of azaallyl anions, generated from glycine Schiff bases, with Ar-acyl halides furnishes N-acylaziridines via intramolecular cyclization.
