Invention Grant
- Patent Title: Process for the preparation of lacosamide
- Patent Title (中): 制备漆酶的方法
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Application No.: US13575152Application Date: 2010-12-22
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Publication No.: US08796488B2Publication Date: 2014-08-05
- Inventor: Alberto Bologna , Patrizia Castoldi , Domenico Vergani , Giorgio Bertolini
- Applicant: Alberto Bologna , Patrizia Castoldi , Domenico Vergani , Giorgio Bertolini
- Applicant Address: IT Milan
- Assignee: Euticals S.p.A.
- Current Assignee: Euticals S.p.A.
- Current Assignee Address: IT Milan
- Agency: Hueschen and Sage
- Priority: ITMI2010A0127 20100129
- International Application: PCT/IB2010/056014 WO 20101222
- International Announcement: WO2011/092559 WO 20110804
- Main IPC: C07C233/06
- IPC: C07C233/06 ; C07C231/14 ; C07C231/20 ; C07C231/12 ; C07C237/22 ; C07C237/06

Abstract:
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.
Public/Granted literature
- US20130030216A1 PROCESS FOR THE PREPARATION OF LACOSAMIDE Public/Granted day:2013-01-31
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