📜N-甲基-3-(1,2,3,6-四氢-1-甲基-4-吡啶)-1H-吲哚-5-乙烷磺酰胺置于palladium 10% On Activated Carbon 盐酸,氢气,溶剂黄146体系中,用 异丙醇,丙酮 用作溶剂,5.0~25.0 °C,289.59 Kpa 条件下,反应生成盐酸那拉曲坦 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-2010062970-A1 优先权日:2006-08-18 标题 :Synthesis of propyl phenoxy ethers and use as delivery agents
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-2008022242-A2 优先权日:2006-08-18 标 题:Synthesis of propyl phenoxy ethers and use as delivery agents
专利号:EP-2053918-A2 优先权日:2006-08-18 标 题 :Synthesis of propyl phenoxy ethers and use as delivery agents