公开(公告)号：US08426612B2

公开(公告)日：2013-04-23

申请号：US12995390

申请日：2009-11-09

申请人： Siro Serafini ,  Andrea Castellin ,  Claudio Dal Santo

发明人： Siro Serafini ,  Andrea Castellin ,  Claudio Dal Santo

IPC分类号： C07D209/04

CPC分类号： C07D403/06

摘要： The present invention refers to the synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole, a drug known by the name Eletriptan, or of its salts. In particular, the present invention regards a process for the synthesis of Eletriptan or of its salt, comprising the following steps: a) Salifying the intermediate of Formula (6), using a dicarboxylic acid to obtain a derived salt; b) Optionally, purifying said raw salt obtained according to step a) by solvent crystallization to obtain a purified salt of the intermediate of Formula (6); c) Converting said salt of the intermediate of formula (6) according to step a) or said purified salt according to step b) into an intermediate of formula (10); d) Converting the intermediate of Formula (10) into Eletriptan or its salt.

摘要翻译： 本发明涉及合成名为Eletriptan的3 - {[（2R）-1-甲基吡咯烷-2-基]甲基} -5- [2-（苯基磺酰基）乙基] -1H-吲哚， 或其盐。 特别地，本发明涉及一种合成埃曲普坦或其盐的方法，包括以下步骤：a）使用二羧酸使式（6）的中间体盐化得到衍生的盐; b）任选地，通过溶剂结晶纯化根据步骤a）获得的所述生盐，得到式（6）中间体的纯化盐; c）根据步骤a）将所述式（6）的中间体的盐或根据步骤b）的所述纯化盐转化成式（10）的中间体; d）将式（10）的中间体转化成Eletriptan或其盐。

公开(公告)号：US20110166364A1

公开(公告)日：2011-07-07

申请号：US12995390

申请日：2009-11-09

申请人： Siro Serafini ,  Andrea Castellin ,  Claudio Dal Santo

发明人： Siro Serafini ,  Andrea Castellin ,  Claudio Dal Santo

IPC分类号： C07D403/06

CPC分类号： C07D403/06

摘要： The present invention refers to the synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole, a drug known by the name Eletriptan, or of its salts. In particular, the present invention regards a process for the synthesis of Eletriptan or of its salt, comprising the following steps: a) Salifying the intermediate of Formula (6), using a dicarboxylic acid to obtain a derived salt; b) Optionally, purifying said raw salt obtained according to step a) by solvent crystallization to obtain a purified salt of the intermediate of Formula (6); c) Converting said salt of the intermediate of formula (6) according to step a) or said purified salt according to step b) into an intermediate of formula (10); d) Converting the intermediate of Formula (10) into Eletriptan or its salt.

摘要翻译： 本发明涉及合成名为Eletriptan的3 - {[（2R）-1-甲基吡咯烷-2-基]甲基} -5- [2-（苯基磺酰基）乙基] -1H-吲哚， 或其盐。 特别地，本发明涉及一种合成埃曲普坦或其盐的方法，包括以下步骤：a）使用二羧酸使式（6）的中间体盐化得到衍生的盐; b）任选地，通过溶剂结晶纯化根据步骤a）获得的所述生盐，得到式（6）中间体的纯化盐; c）根据步骤a）将所述式（6）的中间体的盐或根据步骤b）的所述纯化盐转化成式（10）的中间体; d）将式（10）的中间体转化成Eletriptan或其盐。

公开(公告)号：US5550287A

公开(公告)日：1996-08-27

申请号：US397955

申请日：1995-03-03

申请人： Vincenzo Cannata ,  Valeriano Merli ,  Claudio Dal Santo

发明人： Vincenzo Cannata ,  Valeriano Merli ,  Claudio Dal Santo

IPC分类号： A61K49/04 ,  B01D15/08 ,  C07C231/12 ,  C07C231/22 ,  C07C231/24 ,  C07C233/05 ,  C07C237/46

CPC分类号： C07C231/12 ,  C07C231/24 ,  C07C237/46

摘要： A process for the preparation and purification of L-5-(2-hydroxypropionylamino)-2,4,6-triiodoisophthalic acid bis-(1,3-dihydroxypropylamide) by using ion-exchange resins is described.

摘要翻译： 描述了使用离子交换树脂制备和纯化L-5-（2-羟基丙酰基氨基）-2,4,6-三碘代邻苯二甲酸双 - （1,3-二羟丙基酰胺）的方法。