公开(公告)号：EP1162202A1

公开(公告)日：2001-12-12

申请号：EP00909370.9

申请日：2000-03-13

申请人： Medichem S.A.

发明人： ARNALOT I AGUILAR, Carmen ,  BOSCH I LLAD , Jordi ,  ONRUBIA MIGUEL, M Carmen

IPC分类号： C07D405/12

CPC分类号： C07D405/12

摘要： The invention discloses a process for the preparation of the polymorph A of doxazosin mesylate, consisting essentially of reacting doxazosin base with methanesulfonic acid in a mixture of solvents containing an alcohol and a chlorinated solvent, subsequently removing the chlorinated solvent by distillation and precipitating the desired product in an alcohol, after heating the suspension formed to the reflux temperature of the solvent.

摘要翻译： 本发明公开了一种制备甲磺酸多沙唑嗪的多晶型物A的方法，其基本上由多沙唑嗪碱与甲磺酸在含有醇和氯化溶剂的溶剂的混合物中反应，随后通过蒸馏除去氯化溶剂并沉淀所需产物 在醇中，将形成的悬浮液加热至溶剂的回流温度。

公开(公告)号：EP1213279B1

公开(公告)日：2004-09-15

申请号：EP00945958.7

申请日：2000-07-17

申请人： Medichem S.A.

发明人： ARNALOT I AGUILAR, Carmen ,  BOSCH I LLADO, Jordi ,  CAMPS GARCIA, Pelayo ,  ONRUBIA MIGUEL, Maria del Carmen ,  SOLDEVILLA MADRID, Nuria

IPC分类号： C07C213/08 ,  C07C217/74

CPC分类号： C07C213/08 ,  C07C217/74 ,  C07C2601/14

摘要： Process for producing venlafaxine and/or physiologically acceptable addition salts thereof, consisting in reacting a compound having the general formula (II) wherein R is a C1-C10 alkyl group, aryl group, aralkyl group or cycloalkyl group having from 3 to 6 carbon atoms, with an organomagnesian compound having the general formula (III) wherein X is a halogen atom and, if desired, a salt of venlafaxine can be obtained by reaction with a physiologically acceptable acid.

摘要翻译： 一种制备文拉法辛和/或其生理上可接受的加成盐的方法，其通过使通式（II）的化合物反应，其中R是3至6个碳原子的C 1 -C 10烷基，芳基，芳烷基或环烷基 与通式（III）的有机镁化合物，其中X是卤素原子，如果需要，通过与生理上可接受的酸反应形成所得文拉法新的盐。

公开(公告)号：EP1162202B1

公开(公告)日：2002-10-23

申请号：EP00909370.9

申请日：2000-03-13

申请人： Medichem S.A.

发明人： ARNALOT I AGUILAR, Carmen ,  BOSCH I LLADO, Jordi ,  ONRUBIA MIGUEL, M Carmen

IPC分类号： C07D405/12

CPC分类号： C07D405/12

摘要： The invention relates to a method for obtaining polymorph A from doxazosine mesylate, essentially consisting in reacting the basic doxazosine with methanesulphonic acid in a mixture of solvents containing an alcohol and a chlorinated solvent, subsequently eliminating the chlorinated solvent by distillation and precipitating the desired product in an alcohol after previously heating the resulting suspension to solvent reflux temperature.

公开(公告)号：EP1213279A1

公开(公告)日：2002-06-12

申请号：EP00945958.7

申请日：2000-07-17

申请人： Medichem S.A.

发明人： ARNALOT I AGUILAR, Carmen ,  BOSCH I LLADO, Jordi ,  CAMPS GARCIA, Pelayo ,  ONRUBIA MIGUEL, Maria del Carmen ,  SOLDEVILLA MADRID, Nuria

IPC分类号： C07C213/08 ,  C07C217/74

CPC分类号： C07C213/08 ,  C07C217/74 ,  C07C2601/14

摘要： A process for the preparation of venlafaxin and/or the physiologically acceptable addition salts thereof that consists of reacting a compound of general formula (II) where R is a C 1 -C 10 alkyl, aryl, aralkyl or cycloalkyl group of 3 to 6 atoms of carbon, with a organomagnesium compound of general formula (III) where X is an atom of halogen and, if desired, a salt of the thus obtained venlafaxin is formed by reaction thereof with a physiologically acceptable acid.