CAS: 143322-58-1; Eletriptan

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CAS号1225327-17-2 (R)-benzyl 2-(5... | CAS号1162655-06-2 3-[[(R)-1-methy... | CAS号180637-89-2 (R)-3-[(1-甲基-2-... | CAS号75-75-2 甲基磺酸 | CAS号5535-48-8 苯基乙烯基砜 | CAS号10075-50-0 5-溴吲哚 | CAS号143322-57-0 (R)-5-溴-3-(1-甲基... | CAS号1225327-16-1 5-(2-(phenylsul... | CAS号177834-92-3 依来曲普坦氢溴酸盐

(E)-5-(2-(Phenylsulfonyl)Vinyl)-1H-Indole置于palladium 10% On Activated Carbon Lithium Aluminium Tetrahydride,甲烷磺酸,乙基溴化镁,氢气体系中,用 四氢呋喃,甲醇,乙醚,二氯甲烷,丙酮 用作溶剂,-25.0~5.0 °C,344.75 Kpa 条件下,反应 10.5H,反应生成依来曲普坦
参考文献:Novel Process For The Preparation Of Eletriptan
标题:Novel Process For The Preparation Of Eletriptan
摘要:这项发明涉及一种新型制备(R)-3-((1-甲基吡咯烷-2-基)甲基)-5-(2-(苯磺酰基)乙基)-1H-吲哚及其中间体的方法.

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:US-10173993-B2
优先权日:2015-12-09
标题 :Process for the synthesis of sulfones and sulfonamides
发明人：VON WOLFF NIKLAS; CHAR JOËLLE; CANTAT THIBAULT
权利人:COMMISSARIAT ENERGIE ATOMIQUE
摘要:A one pot single step process is described for the synthesis of a compound, including a labeled compound, containing a sulfonyl functional group comprising the step of mixing together a silane, an SO 2 source, an electrophilic compound, an activating compound and optionally a metal catalyst. A process for producing tracers from a labeled sulfonyl containing compound prepared by the described process is also included.

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:US-11897827-B1
优先权日:2022-11-22
标 题 :Carbon isotope exchange mediated by vanadium complexes
发明人：BUKHRYAKOV KONSTANTIN
权利人:BUKHRYAKOV KONSTANTIN; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES
摘要:The subject invention provides catalytical compounds/complexes, compositions comprising such compound/complex, synthesis of the compounds/complexes, and methods of using such compounds/complexes as catalysts in, for example, carbon isotope exchange (CIE) on target bioactive molecules. Methods that allow CIE directly on drug candidates are of great importance to chemistry, biology, and medicine. Especially valuable are catalytic procedures that rely on a limited collection of available labeled materials. The instant method comprises converting a methyl group to terminal â•?CH2 utilizing transfer dehydrogenation catalysts to enable V-based olefin metathesis, followed by a hydrogenation step. The one-pot strategy allows the formal methylation/demethylation sequence and can be applied to an assortment of alkyl-containing compounds.

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.