CAS: 177834-92-3; Eletriptan Hydrobromide

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(R)-5-(2-Phenylsulphonylethenyl)-3-(N-甲基吡咯烷-2-基-甲基)-1H-吲哚氢溴酸盐置于钯 甲醇体系中,用 甲醇,异丙醇 用作溶剂,25.0~45.0 °C,64.35 Mpa 条件下,反应 10.5H,反应生成依来曲普坦氢溴酸盐
参考文献:Process For Preparation Of Eletriptan And Salt Thereof
标题:Process For Preparation Of Eletriptan And Salt Thereof
摘要:本发明涉及一种改进的制备3-(N-甲基-2(R)-吡咯烷基)-5-[2-(苯基磺酰基)乙基]-1H-吲哚或其药学上可接受的盐,特别是3-(N-甲基-2(R)-吡咯烷基)-5-[2-(苯基磺酰基)乙基]-1H-吲哚盐酸盐(盐酸厄洛替普坦).本发明还涉及3-(N-甲基-2(R)-吡咯烷基)-5-[2-(苯基磺酰基)乙烯基]-1H-吲哚盐酸盐的新型多晶形态及其制备方法.

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-2005103035-A1
优先权日:2004-04-23
标题:Modified fischer indole synthesis of eletriptan
发明人：ASHCROFT CHRISTOPHER PAUL
权利人:PFIZER LTD; ASHCROFT CHRISTOPHER PAUL; PFIZER
摘要:The present invention relates to a new process for the preparation of eletriptan (I), or its enantiomer comprising a modified Fischer indole synthesis, namely the reaction of a compound of formula (II), wherein R1 is a suitable hydrazine protecting group, with a compound of formula (III) wherein R2 is an aldehyde group (-CHO) or the functional equivalent thereof.

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-2015071831-A1
优先权日:2013-11-18
标 题 :An improved process for minimising the formation of dehalogenated byproducts
发明人：KADAM SHASHIKANT; ARADDY RAJSHEKAR; KONDRAGUNTA VENKATESWARA RAO; HULAVALE YOGESH; SOMISETTI NARENDER RAO; CHENNAMSETTY SUNEEL MANOHAR BABU; HARIHARAN SIVARAMAKRISHNAN
权利人:PIRAMAL ENTPR LTD
摘要:The present invention provides an improved process for preparation of organic compounds represented by Formula-Z; wherein effectively minimising the formation of dehalogenated by-products is achieved. In the process, the reduction is carried out using suitable reducing agent; more preferably Lithium Aluminium Hydride (LAH) in a solvent system, wherein at least one of the solvent is selected from halogenated solvents, which acts as co-solvent. The process of the present invention is useful for minimising of the formation of dehalogenated by-products during synthesis of various active pharmaceutical ingredients such as Paroxetine Hydrochloride, Cinacalcet, Eletriptan and Asenapine.

专利号:US-2010062970-A1
优先权日:2006-08-18
标题 :Synthesis of propyl phenoxy ethers and use as delivery agents

专利号:UA-68402-C2
优先权日:1998-11-27
标 题 :Eletriptan hydrobromide monohydrate, pharmaceutical composition, method of treatment (variants), method for synthesis of eletriptan hydrobromide monohydrate (variants) and method for preparing anhydrous eletriptan hydrobromide