📜N,N-二甲基色胺置于三乙基硅烷,Sodium Tungstate,硫酸,双氧水,三溴化硼,三氟乙酸体系中,用 甲醇,二氯甲烷,水,甲苯 作为反应溶剂,化学反应 37.33H,反应生成 蟾毒色胺 参考文献:The Chemistry Of Indoles. Ciii. Simple Syntheses Of Serotonin,N-Methylserotonin,Bufotenine,5-Methoxy-N-Methyltryptamine,Bufobutanoic Acid,N-(Indol-3-yl)Methyl-5-Methoxy-N-Methyltryptamine,And Lespedamine Based On 1-Hydroxyindole Chemistry. 标题:The Chemistry Of Indoles. Ciii. Simple Syntheses Of Serotonin,N-Methylserotonin,Bufotenine,5-Methoxy-N-Methyltryptamine,Bufobutanoic Acid,N-(Indol-3-yl)Methyl-5-Methoxy-N-Methyltryptamine,And Lespedamine Based On 1-Hydroxyindole Chemistry. 摘要:本文描述了利用1-羟色胺的选择性亲核取代反应,合成新型简单物质的方法,这些物质包括:血清素(1A),N-甲基血清素(1B),蟾毒色胺(1C),5-甲氧基-N-甲基色胺(2A),蟾毒色酸(3A),N-(吲哚-3-基)甲基-5-甲氧基-N-甲基色胺(4)和莱斯佩达明(5).此外,还报道了有效的5-苄氧基色胺和1-甲氧基-2-氧吲哚合成方法. DOI:10.1248/cpb.49.87
专利号:US-11912647-B2 优先权日:2020-05-22 标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation 发明人:CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS 权利人:UNIV GEORGIA 摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.
专利号:US-2025305018-A1 优先权日:2022-05-09 标题 :Synthesis of glycosylated hydroxytryptamine compounds and methods of their use 发明人:MORRISON JAMES 权利人:CY BIOPHARMA AG 摘要:Provided herein is a method of treating a disorder (e.g. depression, anxiety, pain, inflammation, or addiction), or symptoms thereof, by administering an effective amount of a glycosylated hydroxytryptamine compound, such as compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is a glycosyl group and the other variables are as defined herein. Also provided herein is a method of enzymatically synthesizing the glycosylated hydroxytryptamine compounds.
专利号:EP-4522760-A2 优先权日:2022-05-09 标题 :Synthesis of glycosylated hydroxytryptamine compounds and methods of their use
专利号:WO-2025169153-A1 优先权日:2024-02-07 标题:Making 5-methoxy-n,n-dimethyltryptamine and bufotenin 发明人:HOMON ANTON; LARAMIE JAXON; HAYWARD JOHN; TRANT JOHN 权利人:HUXLEY HEALTH INC 摘要:Disclosed is a process for, starting from melatonin, the synthesis of 2-(5-methoxy-lH-indol-3-yl)-N,Ndimethylethan-l-amine (MeO-DMT) or a bufotenin salt, said process involving nucleophilic de-acetylation, contacting the resulting 2-(5-methoxy-lH-indol-3-yl)ethan-l-amine with an aryloxy or alkoxy-carbonylation reagent to form a first carbamate, reducing the carbamate, adding a second aryloxy or alkoxy carbonylation reagent to form a second carbamate and reducing said second carbamate to form MeO-DMT followed by the addition of boron tribromide to MeO-DMT in dichloromethane to form bufotenin hydrobromide.
专利号:CN-117597329-A 优先权日:2021-05-05 标题:Method for the catalytic synthesis of tryptamine and precursors thereof
专利号:US-2021363098-A1 优先权日:2020-05-22 标题 :Diversity-oriented synthesis of n,n,o-trisubstituted hydroxylamines from alcohols and amines by n-o bond formation