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1. 发明申请

US20050240018A1 Process for the production of n-(2,6-dimethyl-phenyl)-2-piperazin-1-yl-acetamide 有权
标题翻译：制备正 - （2,6-二甲基 - 苯基）-2-哌嗪-1-基 - 乙酰胺的方法
公开(公告)号：US20050240018A1
公开(公告)日：2005-10-27
申请号：US10518887
申请日：2003-06-19
申请人： Michel Joseph Maurice Guillaume , Josef Ludo Jan Cuypers , Ivan Joseph Maria Vervest , Stefan Marcel Herman Leurs , Dirk De Smaele
发明人： Michel Joseph Maurice Guillaume , Josef Ludo Jan Cuypers , Ivan Joseph Maria Vervest , Stefan Marcel Herman Leurs , Dirk De Smaele
IPC分类号： C07D295/14 , C07D295/15 , C07D241/04
CPC分类号： C07D295/15
摘要： 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).
摘要翻译：本发明涉及一种适用于生产由反应得到的N-（2,6-二甲基 - 苯基）-2-哌嗪-1-基 - 乙酰胺（也称为N-利多卡因）的工业开发的新方法的哌嗪与N-卤代乙酰基-2,6-二甲苯胺。该方法包括连续步骤a）至f）a）使哌嗪与N-卤代乙酰基-2,6-二甲苯胺在摩尔比为约1/1至约6/1之间的水溶液中溶解等摩尔量 HCl量; b）将步骤a）中形成的固体与反应混合物分离; c）中和滤液; d）用与步骤a）中提及的水性溶剂不混合的溶剂萃取滤液; e）从步骤d）中所述的溶剂中结晶出N-（2,6-二甲基 - 苯基）-2-哌嗪-1-基 - 乙酰胺，和f）将步骤e）中获得的固体与步骤 d）。

2. 发明授权

US08541578B2 Process for the production of n-(2,6-dimethyl-phenyl)-2-piperazin-1-yl-acetamide 有权
标题翻译：制备正 - （2,6-二甲基 - 苯基）-2-哌嗪-1-基 - 乙酰胺的方法
公开(公告)号：US08541578B2
公开(公告)日：2013-09-24
申请号：US10518887
申请日：2003-06-19
申请人： Michel Joseph Maurice André Guillaume , Jozef Ludo Jan Cuypers , Ivan Joseph Maria Vervest , Stefan Marcel Herman Leurs , Dirk De Smaele
发明人： Michel Joseph Maurice André Guillaume , Jozef Ludo Jan Cuypers , Ivan Joseph Maria Vervest , Stefan Marcel Herman Leurs , Dirk De Smaele
IPC分类号： C07D241/00 , C07D241/02
CPC分类号： C07D295/15
摘要： 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).
摘要翻译：本发明涉及一种适用于生产由反应得到的N-（2,6-二甲基 - 苯基）-2-哌嗪-1-基 - 乙酰胺（也称为N-利多卡因）的工业开发的新方法的哌嗪与N-卤代乙酰基-2,6-二甲苯胺。该方法包括连续步骤a）至f）a）使哌嗪与N-卤代乙酰基-2,6-二甲苯胺在摩尔比为约1/1至约6/1之间的水溶液中溶解等摩尔量 HCl量; b）将步骤a）中形成的固体与反应混合物分离; c）中和滤液; d）用与步骤a）中提及的水性溶剂不混合的溶剂萃取滤液; e）从步骤d）中所述的溶剂中结晶出N-（2,6-二甲基 - 苯基）-2-哌嗪-1-基 - 乙酰胺，和f）将步骤e）中获得的固体与步骤 d）。

3. 发明授权

US09006422B2 Oxidation process for preparing 3-formyl-cephem derivatives 有权
标题翻译：制备3-甲酰基头孢烯衍生物的氧化方法
公开(公告)号：US09006422B2
公开(公告)日：2015-04-14
申请号：US13696151
申请日：2011-05-09
申请人： Ivan Joseph Maria Vervest
发明人： Ivan Joseph Maria Vervest
IPC分类号： C07D501/34
CPC分类号： C07D501/04 , C07D501/34
摘要： The present invention relates to an improved process for oxidizing 3-hydroxy-methyl-cephem derivatives to the corresponding 3-formyl-cephem derivatives. In particular this oxidation process is for the preparation of 7-[2-(5-amino-[1,2,4]thia-diazol-3-yl)-2-hydroxyimino-acetylamino]-3-formyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid derivatives of formula (I) using a combination of a hypervalent iodine oxidizing agent of the type 10-I-3 such as bis(acetoxy)iodo-benzene (BAIB) and a catalyst such as 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO). These compounds of formula (I) are intermediates in the synthesis of ceftobiprole.
摘要翻译：本发明涉及将3-羟基甲基头孢烯衍生物氧化为相应的3-甲酰基头孢烯衍生物的改进方法。特别地，该氧化方法用于制备7- [2-（5-氨基 - [1,2,4]噻二唑-3-基）-2-羟基亚氨基 - 乙酰基氨基] -3-甲酰基-8-氧代 -5-硫杂-1-氮杂 - 双环[4.2.0]辛-2-烯-2-羧酸衍生物，其使用10-I-3型的高价碘氧化剂的组合，例如双（乙酰氧基）碘 - 苯（BAIB）和催化剂如2,2,6,6-四甲基-1-哌啶氧基（TEMPO）。这些式（I）化合物是合成头孢匹罗的中间体。

4. 发明申请

US20130066065A1 OXIDATION PROCESS FOR PREPARING 3-FORMYL-CEPHEM DERIVATIVES 有权
标题翻译：用于制备3-甲基孕酮衍生物的氧化方法
公开(公告)号：US20130066065A1
公开(公告)日：2013-03-14
申请号：US13696151
申请日：2011-05-09
申请人： Ivan Joseph Maria Vervest
发明人： Ivan Joseph Maria Vervest
IPC分类号： C07D501/57
CPC分类号： C07D501/04 , C07D501/34
摘要： The present invention relates to an improved process for oxidizing 3-hydroxy-methyl-cephem derivatives to the corresponding 3-formyl-cephem derivatives. In particular this oxidation process is for the preparation of 7-[2-(5-amino-[1,2,4]thia-diazol-3-yl)-2-hydroxyimino-acetylamino]-3-formyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid derivatives of formula (I) using a combination of a hypervalent iodine oxidizing agent of the type 10-I-3 such as bis(acetoxy)iodo-benzene (BAIB) and a catalyst such as 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO). These compounds of formula (I) are intermediates in the synthesis of ceftobiprole.
摘要翻译：本发明涉及将3-羟基甲基头孢烯衍生物氧化为相应的3-甲酰基头孢烯衍生物的改进方法。特别地，该氧化方法用于制备7- [2-（5-氨基 - [1,2,4]噻二唑-3-基）-2-羟基亚氨基 - 乙酰基氨基] -3-甲酰基-8-氧代 -5-硫杂-1-氮杂 - 双环[4.2.0]辛-2-烯-2-羧酸衍生物，其使用10-I-3型的高价碘氧化剂的组合，例如双（乙酰氧基）碘 - 苯（BAIB）和催化剂如2,2,6,6-四甲基-1-哌啶氧基（TEMPO）。这些式（I）化合物是合成头孢匹罗的中间体。

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