N,N-二甲基-3-氯丙胺,原甲酸三甲酯置于magnesium体系中,用 环己烷 用作溶剂,化学反应 6.0H,反应生成4-二甲胺基丁醛缩二甲醇 参考文献: A Novel Process For Preparation Of Indole Derivatives[fr] Nouveau Procede Pour La Preparation De Derives D'Indole 标题: A Novel Process For Preparation Of Indole Derivatives[fr] Nouveau Procede Pour La Preparation De Derives D'Indole 摘要:一种制备3-(2-二甲胺基)-N-甲基-1H-吲哚-5-甲磺酰胺化合物的新方法,包括将4-氢化-N-甲基苯甲磺酰胺与4-二甲基氨基丁醛二乙基缩醛在氯化溶剂中在乙基聚磷酸存在下反应,并将粗产品转化为3-(2-二甲胺基)-N-甲基-1H-吲哚-5-甲磺酰胺琥珀酸盐的高纯度和颜色的产品.
专利号:US-5808064-A 优先权日:1996-08-13 标题 :Palladium catalyzed indolization 发明人:CHEN CHENG-YI; LARSEN ROBERT D 权利人:MERCK & CO INC 摘要:We have found that 2-unsubstituted indoles of structural formula (IV) can be cost-effectively synthesized in high yield by the palladium-catalyzed coupling/ring closure of a 2-halo or 2-trifluoromethylsulfonyloxy aniline (I) and an acyl silane derivative (II), followed by deprotection of the silyl protecting groups. +TR The process of the present invention is particularly useful to form indoles containing acid-labile substituents such as triazole, acetyl, ketal, cyano, and carbamate, or indoles having a good leaving group in the benzyl position. The advantages of the present process are that it does not require the use of triphenyl phosphine or tetrabutyl ammonium chloride or lithium chloride. When applied to 5-triazolyl substituted indoles, the present process also eliminates the tendency of triazolyl polymerization in the Fischer indole synthesis.
专利号:EP-0925302-B1 优先权日:1996-08-13 标 题:Palladium catalyzed indolization 发明人:CHEN CHENG-YI; LARSEN ROBERT D 权利人:MERCK & CO INC 摘要:We have found that 2-unsubstituted indoles of structural formula (IV) can be cost-effectively synthesized in high yield by the palladium-catalyzed coupling/ring closure of a 2-halo or 2-trifluoromethylsulfonyloxy aniline (I) and an acyl silane derivative (II), followed by deprotection of the silyl protecting groups. The process of the present invention is particularly useful to form indoles containing acid-labile substituents such as triazole, acetyl, ketal, cyano, and carbamate, or indoles having a good leaving group in the benzyl position. The advantages of the present process are that it does not require the use of triphenyl phosphine or tetrabutyl ammonium chloride or lithium chloride. When applied to 5-triazolyl substituted indoles, the present process also eliminates the tendency of triazolyl polymerization in the Fischer indole synthesis. Still further, the present invention is also directed to the novel intermediates of structural formulae (V) and (VI).
专利号:US-2025101038-A1 优先权日:2021-12-24 标 题 :Compounds 发明人:BANISTER SAMUEL; JORGENSEN WILLIAM; TAN JINLONG 权利人:Psylo Pty Ltd 摘要:The present disclosure relates generally to compounds, their methods of synthesis, and their use in the treatment of mental illness or central nervous system disorders.
专利号:CN-115417859-B 优先权日:2022-09-19 标 题:Synthesis method of rizatriptan benzoate