CAS: 175481-36-4; (2R)-2-Acetamido-N-Benzyl-3-Methoxypropanamide

上下游产品

(R,S)-N-acetylserine-N-benzylamide methyl iodide α-acetamido-N-benzyl-α-cyanoacetamide methyl α-acetamido-N-benzylmalonamate(2S)-2-(acetylamino)-N-benzyl-3-methoxypropanamide lacosamide N-Benzyl-2-Amino-3-Methoxypropionamide

拉科酰胺外消旋物置于盐酸体系中,用 乙醇,甲基叔丁基醚,水,乙酸乙酯 用作溶剂,化学反应 6.0H,反应生成拉克酰胺
参考文献: Process For The Synthesis Of Lacosamide[fr] Procédé De Synthèse De Lacosamide
标题: Process For The Synthesis Of Lacosamide[fr] Procédé De Synthèse De Lacosamide
摘要:本文介绍了一种使用d,L-丝氨酸作为起始物合成lacosamide的新工艺,其中羟基的甲基化反应使用廉价碱(如naoh)和廉价烷基化剂(无毒且非致癌,如对甲苯磺酸甲酯)进行;在通过酰胺的选择性水解,用手性酸(hx*)在有机溶剂中对外消旋混合物进行盐化,分离非对映体混合物,最好通过沉淀r对映体并随后乙酰化光学纯中间体来分离lacosamide的r对映体.

专利信息

专利号:US-8748660-B2
优先权日:2012-07-09
标题:Process for the synthesis of antiepileptic drug lacosamide
发明人：MURUGAN MUTHUKRISHNAN; MUJAHID MOHAMMAD; MAJUMDAR PRASHANT PRAMOD
权利人:MURUGAN MUTHUKRISHNAN; MUJAHID MOHAMMAD; MAJUMDAR PRASHANT PRAMOD; COUNCIL SCIENT IND RES
摘要:The present invention relates to the improved and efficient process for the synthesis of antiepileptic drug Lacosamide in high enantiopurity (>98% ee) and better yield. More particularly, the present invention relates to improved and efficient, cost effective process for synthesis of desired (R) isomer of Lacosamide starting from commercially available (S)-benzyl glycidyl ether.

专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:US-10414720-B2
优先权日:2016-09-28
标题:Process for the preparation of lacosamide
发明人：SATHE DHANANJAY G; DAS ARIJIT; Raikar Sanjay; BHAGWATKAR RAHUL; AHIRE RAMDAS
权利人:UNICHEM LAB LTD
摘要: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.

专利号:US-8796488-B2
优先权日:2010-01-29
标 题:Process for the preparation of lacosamide
发明人：BOLOGNA ALBERTO; CASTOLDI PATRIZIA; VERGANI DOMENICO; BERTOLINI GIORGIO
权利人:BOLOGNA ALBERTO; CASTOLDI PATRIZIA; VERGANI DOMENICO; BERTOLINI GIORGIO; EUTICALS SPA
摘要:A novel process for the synthesis of Lacosamide using D,L-serine as starting material is described, where the methylation reaction of hydroxyl is carried out using an inexpensive base such as NaOH and an inexpensive alkylating agent, non-toxic and non-carcinogenic, such as methyl p-toluenesulfonate; the R enantiomer is isolated from the racemic mixture of Lacosamide after selective hydrolysis of the acetamide, salification of the racemic mixture with a chiral acid (HX*) in an organic solvent, resolution of the diastereoisomeric mixture, preferably by precipitation of the R enantiomer, and subsequent acetylation of the optically pure intermediate.

专利号:WO-2024077428-A1
优先权日:2022-10-10
标题 :Enzyme with d-amino acid synthesis activity and use thereof
发明人：PI LI; HUANG ZHIHUA; Zha Liyan; SU HAIXIA; SUN YUE; LIN LICHUN; LI KUN; TANG PENG; WANG JIONG; CHEN LEI; LI XIAOBO; WEI ZIXIANG; XING PANPAN; LIU JIN; WANG XIAOMENG; ZHU CHENGJUN; ZHANG TING
权利人:WUHAN GRAND HOYO CO LTD
摘要:Provided is an enzyme with D-amino acid synthesis activity. The enzyme has an amino acid sequence as shown in SEQ ID NO: 10. Compared with an original strain before mutation, the enzyme has a higher catalytic activity for D-amino acid synthesis, a higher enzyme activity and a higher conversion rate of D-amino acid, and remains more than 76% active in the pH 4-9 range.

专利号:US-2018370905-A1
优先权日:2013-04-05
标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same