CAS: 188113-71-5; 1-[3-[[(2R)-1-Methyl-2-Pyrrolidinyl]Methyl]-5-[(1E)-2-(Phenylsulfonyl)Ethenyl]-1H-Indol-1-Yl]Ethanone

上下游产品

(R)-N-乙酰基-5-溴-3-(N-甲基吡咯烷-2-基甲基)-1H-吲哚 (R)-1-Acetyl-5-Bromo-3-(N-Methylpyrrolidin-2-Ylmethyl)-1H-Indole 205369-12-6
(R)-5-溴-3-(1-甲基-2-吡咯烷基甲基)-1H-吲哚 (R)-5-Bromo-3-(N-Methylpyrrolidine-2-Ylmethyl)-1H-Indole 143322-57-0
(R)-2-[(5-溴-1H-吲哚-3-基)羰基]-1-吡咯烷甲酸苄酯 (R)-3-[(N-Benzyloxycarbonylpyrrolidin-2-yl)Carbonyl]-5-Bromo-1H-Indole 143322-56-9

📜N-苄氧羰基-D-脯氨酸置于palladium Diacetate,三(邻甲基苯基)磷 Lithium Aluminium Tetrahydride,草酰氯,甲基氯化镁,三乙胺,Potassium Hydroxide体系中,用 四氢呋喃,甲基叔丁基醚,水,N,N-二甲基甲酰胺,异丙醇,甲苯 用作溶剂,化学反应 20.5H,反应生成(R,E)-1-(3-((1-甲基吡咯烷-2-基)甲基)-5-(2-(苯基磺酰基)乙烯基)-1H-吲哚-1-基)乙-1-酮
参考文献:Synthesis Of 3--5-[2-(Phenylsulfonyl)Ethyl]-1H-Indole
标题:Synthesis Of 3--5-[2-(Phenylsulfonyl)Ethyl]-1H-Indole
摘要:本发明涉及合成3-{[(2R)-1-甲基吡咯烷-2-基]甲基}-5-[2-(苯磺酰基)乙基]-1H-吲哚,一种以eletriptan命名的药物或其盐.具体而言,本发明涉及一种用于合成eletriptan或其盐的方法,包括以下步骤:A) 用二羧酸盐化式(6)的中间体,以获得衍生盐;B) 可选地,通过溶剂结晶纯化根据步骤a)获得的原始盐,以获得式(6)的中间体的纯化盐;C) 将根据步骤a)获得的式(6)的中间体的盐或根据步骤b)获得的纯化盐转化为式(10)的中间体;D) 将式(10)的中间体转化为eletriptan或其盐.

专利信息

专利号:US-8426612-B2
优先权日:2009-04-22
标 题:Synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5[2-(phenylsulfonyl)ethyl]-1H-indole
发明人：SERAFINI SIRO; CASTELLIN ANDREA; DAL SANTO CLAUDIO
权利人:SERAFINI SIRO; CASTELLIN ANDREA; DAL SANTO CLAUDIO; ITALIANA SINT SPA
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.

专利号:WO-2010121673-A1
优先权日:2009-04-22
标 题 :Synthesis of 3-{[(2r)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1h-indole

专利号:JP-2012524736-A
优先权日:2009-04-22
标 题 :Synthesis of 3-{[(2R) -1-methylpyrrolidin-2-yl] methyl} -5- [2- (phenylsulfonyl) ethyl] 1H-indole

专利号:US-2011166364-A1
优先权日:2009-04-22
标 题 :Synthesis of 3--5-[2-(phenylsulfonyl)ethyl]-1h-indole

专利号:EP-2421853-B1
优先权日:2009-04-22
标 题:Synthesis of 3-{[(2r)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1h-indole

专利号:EP-2421853-A1
优先权日:2009-04-22
标题:Synthesis of 3-{[(2r)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1h-indole