Invention Grant
US08541578B2 Process for the production of n-(2,6-dimethyl-phenyl)-2-piperazin-1-yl-acetamide
有权
制备正 - (2,6-二甲基 - 苯基)-2-哌嗪-1-基 - 乙酰胺的方法
- Patent Title: Process for the production of n-(2,6-dimethyl-phenyl)-2-piperazin-1-yl-acetamide
- Patent Title (中): 制备正 - (2,6-二甲基 - 苯基)-2-哌嗪-1-基 - 乙酰胺的方法
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Application No.: US10518887Application Date: 2003-06-19
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Publication No.: US08541578B2Publication Date: 2013-09-24
- Inventor: Michel Joseph Maurice André Guillaume , Jozef Ludo Jan Cuypers , Ivan Joseph Maria Vervest , Stefan Marcel Herman Leurs , Dirk De Smaele
- Applicant: Michel Joseph Maurice André Guillaume , Jozef Ludo Jan Cuypers , Ivan Joseph Maria Vervest , Stefan Marcel Herman Leurs , Dirk De Smaele
- Applicant Address: BE Beerse
- Assignee: Janssen Pharmaceutica, N.V.
- Current Assignee: Janssen Pharmaceutica, N.V.
- Current Assignee Address: BE Beerse
- Agent Kiera K. Mathey
- Priority: EP02077749 20020624
- International Application: PCT/EP03/50241 WO 20030619
- International Announcement: WO04/000824 WO 20031231
- Main IPC: C07D241/00
- IPC: C07D241/00 ; C07D241/02

Abstract:
The present invention relates to a novel process, suitable for industrial exploitation for the production of N-(2,6-dimethyl-phenyl)-2-piperazin-1-yl-acetamide, also known as N-lidocaine, obtained from the reaction of piperazine with N-haloacetyl-2,6-xylidine. The process comprises the consecutive steps a) through f) a) reacting piperazine with N-haloacetyl-2,6-xylidine in a molar ratio between about 1/1 and about 6/1 in an aqueous solvent in which has been dissolved an equimolar amount of HCl; b) separating the solid formed in step a) from the reaction mixture; c) neutralizing the filtrate; d) extracting the filtrate with a solvent which is not or only to a small extent miscible with the aqueous solvent mentioned in step a); e) crystallizing the N-(2,6-dimethyl-phenyl)-2-piperazin-1-yl-acetamide from the solvent mentioned in step d) and f) separating the solid obtained in step e) from the solvent mentioned in step d).
Public/Granted literature
- US20050240018A1 Process for the production of n-(2,6-dimethyl-phenyl)-2-piperazin-1-yl-acetamide Public/Granted day:2005-10-27
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