CAS: 143322-57-0; (R)-5-Bromo-3-[(1-Methyl-2-Pyrrolidinyl)Methyl]-1H-Indole

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(R)-2-(5-溴-1H-吲哚-3-羰基)吡咯烷-1-羧酸苯酯置于红铝,Sodium Hydroxide体系中,用 甲苯,水 用作溶剂,化学反应生成(R)-5-溴-3-(1-甲基-2-吡咯烷基甲基)-1H-吲哚
参考文献: Process For The Preparation Of 5-Substsituted Indole Derivative[fr] Procédé Pour La Préparation De Dérivé D'Indole Substitué En Position 5
标题: Process For The Preparation Of 5-Substsituted Indole Derivative[fr] Procédé Pour La Préparation De Dérivé D'Indole Substitué En Position 5

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-2012004811-A8
优先权日:2010-07-06
标题:Process for the preparation of 5-substsituted indole derivative
发明人：BHIRUD SHEKHAR BHASKAR; JOHAR PERMINDER SINGH; SHARMA EKTA; PRAJAPATY RAMKARAN; GUPTA CHANDAN KUMAR
权利人:IND SWIFT LAB LTD; BHIRUD SHEKHAR BHASKAR; JOHAR PERMINDER SINGH; SHARMA EKTA; PRAJAPATY RAMKARAN; GUPTA CHANDAN KUMAR
摘要:The present invention relates to an improved and industrially advantageous process for preparation of eletriptan of formula I, or pharmaceutically acceptable salts thereof from bromo indole intermediate of formula II, through isolation of N-acetylated bromo indole intermediate of formula III, to elude carrying forward of impurities to next stage. The present invention relates to process for the preparation of 5-bromo-3-[(R)-1-methyl-pyrrolidin-2-ylmethyl]-1H-indol of formula II, a key intermediate for the synthesis of eletriptan or pharmaceutically acceptable salts thereof, through novel keto carbamate intermediate. The present invention also relates to novel process for the preparation of α-form of eletriptan hydrobromide.

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