4-氨基-N-甲基苯乙基磺酰胺置于copper(L) Iodide,乙醇,Potassium Tert-Butylate,碘,碳酸氢钠,Lithium Chloride,Potassium Hydroxide体系中,用 N-甲基吡咯烷酮,二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 2.5H,反应生成 N-甲基-1H-吲哚-5-乙基磺酰胺 参考文献: A Process For The Synthesis Of Naratriptan[fr] Procédé De Synthèse Du Naratriptan 标题: A Process For The Synthesis Of Naratriptan[fr] Procédé De Synthèse Du Naratriptan
专利号:WO-2008056378-A3 优先权日:2006-11-09 标 题:Novel process for the preparation of naratriptan hydrochloride 发明人:PULLA REDDY MUDDASANI; RAJASEKHARA REDDY PEDDI; VENKAIAH CHOWDARY NANNAPANENI 权利人:NATCO PHARMA LTD; PULLA REDDY MUDDASANI; RAJASEKHARA REDDY PEDDI; VENKAIAH CHOWDARY NANNAPANENI 摘要:Present invention provides a novel and improved process for the preparation of N- methyl-1H-indole-5-ethanesulfonamide of formula (I). Compound of formula (I) is a key intermediate used in the synthesis of naratriptan hydrochloride of formula (II). Hydrazone derivative of formula (XL) derived from the corresponding hydrazine and pyruvate ester is reacted with an acid catalyst to get the indole-2-carboxylate derivative of formula (XLI). Hydrolysis of this ester and decarboxylation gave the compound of formula (I). Naratriptan hydrochloride (Amerge) is widely used as anti-migraine drug in the market.
专利号:US-8735589-B2 优先权日:2009-08-20 标题:Process for the synthesis of naratriptan 发明人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; CHIKHALIKAR SANDIP VASANT; GHAGARE MARUTI 权利人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; CHIKHALIKAR SANDIP VASANT; GHAGARE MARUTI; CIPLA LTD 摘要:The present invention relates to a process for preparing naratriptan or a salt thereof, the process comprising: (a) reacting a compound of formula (3) with a compound of the formula HCCR n nwherein Z is a protecting group, Y is a leaving group and R is a trialkyl silyl group, a trialkylstannyl group or a zinc (II) halide, to obtain the compound of formula (4); (b) converting the compound of formula (4) to a compound of formula (5)n n nwherein Z′ is hydrogen or a benzyl group; (c) converting the compound of formula (5) to naratriptan; and (d) optionally converting naratriptan to a salt thereof. The present invention also provides novel compounds (3) and (4) and processes for their preparation.
专利号:US-2012220778-A1 优先权日:2009-08-20 标题 :Process for the synthesis of naratriptan
专利号:WO-2010004580-A3 优先权日:2008-07-11 标 题:Process for preparing indole derivatives 发明人:CHIDAMBARAM VENKATESWARAN SRINIVASAN; AGGARWAL ASHVIN KUMAR; WADHWA LALIT 权利人:IND SWIFT LAB LTD; CHIDAMBARAM VENKATESWARAN SRINIVASAN; AGGARWAL ASHVIN KUMAR; WADHWA LALIT 摘要:The present invention provides a process for the preparation of indole derivatives, specifically N - methyl-1H-indole-5-ethanesulfonamide of formula (I), involving novel intermediate, which is used as key intermediate for the synthesis of naratriptan of formula (II), and its pharmaceutically acceptable salts thereof high yield and purity.
专利号:EP-2467373-B1 优先权日:2009-08-20 标 题:A process for the synthesis of naratriptan
专利号:WO-2011021000-A2 优先权日:2009-08-20 标 题:A process for the synthesis of naratriptan
参考标题:The Photoredox-Catalyzed Hydrosulfamoylation Of Styrenes And Its Application In The Novel Synthesis Of Naratriptan 作者:Mingjun Zhang,Miaomiao Chen,Xin Ding,Jin Kang,Yongyue Gao,Xingxing He,Ziwen Wang,Aidang Lu,Qingmin Wang 摘要:The Hydrosulfamoylation Of Diverse Aryl Olefins Provides Facile Access To Alkylsulfonamides. Here We Report A Novel Protocol Utilizing Radical-Mediated Addition And A Thiol-Assisted Strategy To Achieve The Hydrosulfamoylation Of Diverse Styrenes In Modest To Excellent Yields Under Mild And Economic Reaction Conditions. The Methodology Was Found To Provide An Efficient And Convenient Approach For The