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1. 发明授权

EP1614677B1 Improved procedure for the synthesis of bicalutamide 有权
标题翻译：对于比卡鲁胺的制备的改进方法
公开(公告)号：EP1614677B1
公开(公告)日：2009-08-05
申请号：EP05104384.2
申请日：2005-05-24
申请人： Cosma S.p.A.
发明人： Pizzatti, Enrica , Vigano', Enrico , Lussana, Massimiliano , Landonio, Ernesto
IPC分类号： C07C315/02 , C07C319/14 , C07C319/20
CPC分类号： C07C319/20 , C07C315/02 , C07C319/14 , C07C317/46 , C07C323/52 , C07C323/60

2. 发明公开

EP2019096A1 Process for obtaining Cetirizine dihydrochloride 审中-公开
标题翻译： Verfahren zur Gewinnung von Cetirizin-二盐酸盐
公开(公告)号：EP2019096A1
公开(公告)日：2009-01-28
申请号：EP07113218.7
申请日：2007-07-26
申请人： Cosma S.p.A.
发明人： Lussana, Massimiliano , Vigano', Enrico , Pizzatti, Enrica
IPC分类号： C07D295/088
CPC分类号： C07D295/088
摘要： Process for the synthesis of cetirizine dihydrochloride, wherein
(a) a solution of {2-[4-(α-phenyl-p-chlorobenzyl)piperazin-1-yl]}ethanol in 1-7 volumes, referred to the weight of {2-[4-(α-phenyl-p-chlorobenzyl)piperazin-1-yl]}ethanol, of an organic solvent having a boiling point higher than 90°C and being chosen from the group consisting of aliphatic, cycloalifatic or aromatic solvents is provided, whereafter
(b) per equivalent of {2-[4-(α-phenyl-p-chlorobenzyl)piperazin-1-yl]}ethanol employed, 1-2 equivalents of a metal haloacetate or of haloacetic acid, as well as 3-7 equivalents of an alkaly metal hydroxyde are added to the solution as per (a), providing a reaction mixture, where 0,05-0,3 volumes, referred to the weight of {2-[4-(α-phenyl-p-chlorobenzyl)piperazin-1-yl]}ethanol employed, of water and 0,1-1,2 volumes, referred to the weight of {2-(4-(α-phenyl-p-chlorobenzyl)piperazin-1-yl]}ethanol employed, of a polar aprotic, water miscible solvent are added, keeping the internal temperature of the reaction mixture below 60°C, whereafter
(c) the cetirizine base formed within the reaction mixture is converted into its dihydrochloride salt and isolated as such.
摘要翻译：合成西替利嗪二盐酸盐的方法，其中（a）{1-7]体积的{2- [4-（± - 苯基 - 对氯苄基）哌嗪-1-基]}乙醇的溶液称为{ 2- [4-（± - 苯基 - 对氯苄基）哌嗪-1-基]}乙醇，沸点高于90℃的有机溶剂，选自脂肪族，环状芳族或芳族溶剂，然后（b）每当量使用的{2- [4-（± - 苯基 - 对氯苄基）哌嗪-1-基]}乙醇，1-2当量的卤代乙酸金属盐或卤代乙酸，以及根据（a）将3-7当量的烷基金属氢氧化物加入到溶液中，提供反应混合物，其中0.05-0.3体积称为{2- [4-（± - 苯基 - 对氯苄基）哌嗪-1-基]}乙醇，水和0.1-1,2体积，称为{2-（4-（± - 苯基 - 对氯苄基）哌嗪-1-基）吡啶-1-基]}乙醇，加入极性非质子，水混溶性溶剂反应混合物的温度低于60℃，之后（c）将反应混合物内形成的西替利嗪碱转化成其二盐酸盐并将其分离。

3. 发明公开

EP2014644A1 A process for the resolution of racemic verapamil 审中-公开
标题翻译： Verfahren zurLösungvon racemischen维拉帕米
公开(公告)号：EP2014644A1
公开(公告)日：2009-01-14
申请号：EP08157735.5
申请日：2008-06-06
申请人： Cosma S.p.A.
发明人： Bertolotti, Chiara , Lussana, Massimiliano , Pizzatti, Enrica , Vigano', Enrico , Landonio, Ernesto
IPC分类号： C07C253/32 , C07C255/43
CPC分类号： C07C253/34 , C07B57/00 , C07B2200/07 , C07C255/43
摘要： A new process is described for the resolution of racemic verapamil, which allows the desired enantiomer to be obtained in high yields and with high enantiomeric purity. The process uses optically active 2,3-bis[(2-fluorobenzoyl)oxy]butanedioic acid as the resolving agent, and a water/dimethylformamide or water/acetonitrile or water/methanol mixture, as the reaction solvent.
摘要翻译：描述了用于拆分外消旋维拉帕米的新方法，其允许以高产率和高对映体纯度获得所需的对映异构体。该方法使用光学活性2,3-双[（2-氟苯甲酰基）氧基]丁二酸作为拆分剂，和水/二甲基甲酰胺或水/乙腈或水/甲醇混合物作为反应溶剂。

4. 发明公开

EP1900435A1 System for controlling the environmental emissions during the discharge step in centrifuges 审中-公开
标题翻译： Zentrifugenwährenddes Entladungsvorgangs系统zur Steuerung der Umweltemissionen
公开(公告)号：EP1900435A1
公开(公告)日：2008-03-19
申请号：EP06120833.6
申请日：2006-09-18
申请人： Cosma S.p.A.
发明人： Pedretti, Marco
IPC分类号： B04B11/04 , B04B15/08 , B04B7/06 , B04B3/00
CPC分类号： B04B11/04 , B04B3/00 , B04B7/06 , B04B15/08
摘要： A system for controlling the emissions into the environment during the discharge step of a preferably vertical-axis top-load centrifuge (1) comprising a removable bag (12) for containing the material to be centrifuged, and an extraction circuit (2, 3, 4) of the solid part of said material during a discharge step of said bag (12), the extraction circuit (2, 3, 4, 6) is pneumatically connected both to said centrifuge (1) and to said main extraction pipe (4) and the bag (12) present covering means (13) for putting said bag (12) under vacuum with respect to ambient pressure.
摘要翻译：一种用于控制在优选垂直轴上载荷离心机（1）的排放步骤期间排放到环境中的排放系统，该离心机包括用于容纳要离心的材料的可移除袋（12）和提取电路（2,3） 4）在所述袋（12）的排出步骤期间所述材料的实心部分，抽吸回路（2,3,4,6）气动地连接到所述离心机（1）和所述主抽取管（4））和用于将所述袋（12）相对于环境压力放置在真空下的覆盖装置（13）的袋（12）。

5. 发明公开

EP1433784A1 Process for the synthesis of torsemide, in particular of pure and stable form II 审中-公开
标题翻译： Verfahren zur Herstellung von Torsemid，insbesondere von reiner und stableer Form II
公开(公告)号：EP1433784A1
公开(公告)日：2004-06-30
申请号：EP03029586.9
申请日：2003-12-22
申请人： Cosma S.p.A.
发明人： Lusanna, Massimiliano , Rainoni, Mauro , Gambuzza, Filippo
IPC分类号： C07D213/74
CPC分类号： C07D213/74
摘要： The present invention relates to a new process for the synthesis of torsemide, in particular of pure and stable form II, which comprises direct synthesis of torsemide from 4-(3-methylphenylamino)-3-pyridine-sulphonamide. The new process envisages fewer steps than the processes described in the prior art, with improved yields and good quality from the chemical and preferably polymorphous points of view.
摘要翻译：本发明涉及用于合成托塞米特别是纯和稳定形式II的新方法，其包括从4-（3-甲基苯基氨基）-3-吡啶 - 磺酰胺直接合成托塞米。新方法设想比现有技术中描述的方法更少的步骤，具有来自化学和优选多形态观点的改善的产率和良好的质量。

6. 发明公开

EP2805936A1 Process for preparing levomilnacipran HCL 审中-公开
标题翻译： Verfahren zur Herstellung von Levomilnacipran HCL
公开(公告)号：EP2805936A1
公开(公告)日：2014-11-26
申请号：EP13168413.6
申请日：2013-05-20
申请人： Cosma S.p.A.
发明人： Celestini, Paolo , Baretti, Sergio , Pizzatti, Enrica
IPC分类号： C07C231/12 , C07C235/40 , C07C237/24
CPC分类号： C07C231/12 , C07C2601/02 , C07C237/24 , C07C235/40
摘要： The invention relates to one-pot process for preparing (1S,2R)-1-phenyl-1-(N,N-diethylaminocarbonyl)-2-aminomethylcyclopropane of formula (I) comprising the step of reacting (1S,2R)-N,N-diethyl-2-(hydroxymethyl)-1-phenylcyclopropanecarboxamide successively with the following reactants 1) triethyl orthoformate and methanesulfonic acid or triethylamine and methanesulfonyl chloride, 2) a phthalimidating agent, 3) aqueous EtNH 2 , wherein the reaction is carried out in toluene. In another aspect the invention concerns a process for preparing (1S,2R)-N,N-diethyl-2-(hydroxymethyl)-1-phenylcyclopropanecarboxamide trough a step of crystallization of (1S,5R)-1-phenyl-3-oxabicyclo[3.1.0]hexan-2-one.
摘要翻译：本发明涉及一种制备式（I）的（1S，2R）-1-苯基-1-（N，N-二乙基氨基羰基）-2-氨基甲基环丙烷的一锅法，包括使（1S，2R）-N ，N-二乙基-2-（羟甲基）-1-苯基环丙烷甲酰胺依次用以下反应物1）原甲酸三乙酯和甲磺酸或三乙胺和甲磺酰氯，2）苯二酰亚胺化试剂，3）EtNH 2水溶液，其中反应进行在甲苯中。在另一方面，本发明涉及通过（1S，5R）-1-苯基-3-氧杂双环（Ⅲ）的结晶步骤制备（1S，2R）-N，N-二乙基-2-（羟甲基）-1-苯基环丙烷甲酰胺的方法 [3.1.0]己烷-2-酮。

7. 发明公开

EP1614677A3 Improved procedure for the synthesis of bicalutamide 有权
标题翻译：对于比卡鲁胺的制备的改进方法
公开(公告)号：EP1614677A3
公开(公告)日：2006-02-01
申请号：EP05104384.2
申请日：2005-05-24
申请人： Cosma S.p.A.
发明人： Pizzatti, Enrica , Vigano', Enrico , Lussana, Massimiliano , Landonio, Ernesto
IPC分类号： C07C315/02 , C07C319/14 , C07C319/20
CPC分类号： C07C319/20 , C07C315/02 , C07C319/14 , C07C317/46 , C07C323/52 , C07C323/60
摘要： The object of the invention is an improved procedure for the synthesis of bicalutamide, characterised in that the 2-hydroxy-2-methyl-3-(4-fluorophenylthio) propionic acid initially produced undergoes a step to acylate the hydroxyl group in position 2 to give an intermediate 2-acyloxy-2-methyl-3-(4-fluorophenylthio) propionic acid, which allows the formation of a successive N-[4-cyano-3-(trifluoromethyl)-phenyl-]-3-[4-fluorophenylthio]-2-acyloxy-2-methyl-propionamide intermediate.

8. 发明公开

EP1614677A2 Improved procedure for the synthesis of bicalutamide 有权
标题翻译： Verbeetes Verfahren zur Herstellung von Bicalutamid
公开(公告)号：EP1614677A2
公开(公告)日：2006-01-11
申请号：EP05104384.2
申请日：2005-05-24
申请人： Cosma S.p.A.
发明人： Pizzatti, Enrica , Vigano', Enrico , Lussana, Massimiliano , Landonio, Ernesto
IPC分类号： C07C317/00
CPC分类号： C07C319/20 , C07C315/02 , C07C319/14 , C07C317/46 , C07C323/52 , C07C323/60
摘要： The object of the invention is an improved procedure for the synthesis of bicalutamide, characterised in that the 2-hydroxy-2-methyl-3-(4-fluorophenylthio) propionic acid initially produced undergoes a step to acylate the hydroxyl group in position 2 to give an intermediate 2-acyloxy-2-methyl-3-(4-fluorophenylthio) propionic acid, which allows the formation of a successive N-[4-cyano-3-(trifluoromethyl)-phenyl-]-3-[4-fluorophenylthio]-2-acyloxy-2-methyl-propionamide intermediate.
摘要翻译：本发明的目的是用于合成比卡鲁胺的改进方法，其特征在于最初生产的2-羟基-2-甲基-3-（4-氟苯硫基）丙酸经历了将位置2的羟基酰化至得到中间体2-酰氧基-2-甲基-3-（4-氟苯硫基）丙酸，其允许形成连续的N- [4-氰基-3-（三氟甲基） - 苯基] -3- [4- 氟苯硫基] -2-酰氧基-2-甲基 - 丙酰胺中间体。

9. 发明公开

EP3609877A1 NEW PROCESS FOR THE SYNTHESIS OF FIROCOXIB 有权
公开(公告)号：EP3609877A1
公开(公告)日：2020-02-19
申请号：EP17722384.9
申请日：2017-04-14
申请人： Cosma S.p.A.
发明人： CELESTINI, Paolo , BARETTI, Sergio , PIZZATTI, Enrica
IPC分类号： C07D307/60 , C07C323/22

10. 发明公开

EP1767668A1 Method for enamelling cast parts of standard hypoeutectic gray iron 审中-公开
标题翻译： Verfahren zur Emaillierung von Teilen aus hypoeutektischemStandardgrauguß
公开(公告)号：EP1767668A1
公开(公告)日：2007-03-28
申请号：EP05108791.4
申请日：2005-09-23
申请人： Cosma S.p.A.
发明人： Dal Mas, Candido
IPC分类号： C23D5/04
CPC分类号： C23D5/04
摘要： The present invention refers to a method for enamelling cast parts made of standard hypoeutectic gray iron, comprising following steps:
- preparing a cast part of standard hypoeutectic gray iron;
- pre-treating said cast part in order to promote mechanical bond and adherence of the enamel substances to the surface of the part to be enamelled;
- applying porcelain-enamel powders onto the thus pre-treated part by dry electrostatic spray technique;
- vitrifying the enamel powders by exposing the part to a heating and cooling sequence occurring according to such a heating and cooling pattern versus time as to cause the part to dwell at a temperature between 700°C and 780°C for 480 seconds ± 5%.
摘要翻译：本发明涉及一种由标准亚共晶灰铸铁制成的铸件的搪瓷方法，包括以下步骤： - 制备标准亚共晶灰铁铸件; - 预处理所述铸造部件，以促进搪瓷物质的机械粘合和粘附到待搪瓷部件的表面; - 通过干静电喷涂技术将瓷釉粉末涂在预处理部分上; 通过将部件暴露于根据这样的加热和冷却模式发生的加热和冷却模式与时间的关系，使部件在700℃和780℃之间的温度下停留480秒±5％。

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