28920-43-6 = 84418-43-9 反应条件:1.1 Reagents: Ammonium Hydroxide Solvents: Dichloromethane; 0 °C; 0 °C -> Rt 标题:Utility Of 2-Diphenylphosphoryloxy-1,3-Dienes In Multicomponent Hetero-Diels-Alder Reactions To Construct Functionalized Six-Membered Nitrogen Heterocycles 作者:He,Qiuyu; Et Al 参考文献:Chemistry - A European Journal 日期:2022 卷标:28(42)]
125666-68-4 = 84418-43-9 + 115109-65-4 反应条件:1.1 Reagents: Hydrogen Catalysts: Palladium Solvents: Acetic Acid,Water2.1 Reagents: Sodium Hydroxide Solvents: 1,4-Dioxane,Water2.2 Reagents: Hydrochloric Acid Solvents: 1,4-Dioxane,Water 标题:Preparation And Application Of The 5-(4-(9-Fluorenylmethyloxycarbonyl)Aminomethyl-3,5-Dimethoxyphenoxy)-Valeric Acid (Pal) Handle For The Solid-Phase Synthesis Of C-Terminal Peptide Amides Under Mild Conditions 作者:Albericio,Fernando; Et Al 参考文献:Journal Of Organic Chemistry 日期:1990 卷标:55(12) 页码:3730-43]
14660-52-7 + 22080-96-2 = 84418-43-9 + 115109-65-4 反应条件:1.1 Reagents: Potassium Tert-Butoxide Solvents: Dimethylformamide1.2 Solvents: Dimethylformamide2.1 Reagents: Hydroxyamine Hydrochloride Solvents: Pyridine,Water3.1 Reagents: Hydrogen Catalysts: Palladium Solvents: Acetic Acid,Water4.1 Reagents: Sodium Hydroxide Solvents: 1,4-Dioxane,Water4.2 Reagents: Hydrochloric Acid Solvents: 1,4-Dioxane,Water 标题:Preparation And Application Of The 5-(4-(9-Fluorenylmethyloxycarbonyl)Aminomethyl-3,5-Dimethoxyphenoxy)-Valeric Acid (Pal) Handle For The Solid-Phase Synthesis Of C-Terminal Peptide Amides Under Mild Conditions 作者:Albericio,Fernando; Et Al 参考文献:Journal Of Organic Chemistry 日期:1990 卷标:55(12) 页码:3730-43]
28920-43-6 = 84418-43-9 [标题:Reaction Conditions 标题:Facile Sps Of Peptides Having C-Terminal Asn And Gln 作者:Breipohl,Gerhard; Et Al 参考文献:International Journal Of Peptide & Protein Research 日期:1990 卷标:35(3) 页码:281-3]
3019-71-4 + 115134-37-7 = 84418-43-9 反应条件:1.1 Solvents: Dichloromethane; 0 °C; 0 °C -> Rt; Overnight,Rt 标题:Silver-Catalyzed Intermolecular Amination Of C-H Groups 作者:Li,Zigang; Et Al 参考文献:Angewandte Chemie 日期:2007 卷标:46(27) 页码:5184-5186]
125666-69-5 + 28920-44-7 = 84418-43-9 + 115109-65-4 反应条件:1.1 Reagents: Sodium Hydroxide Solvents: 1,4-Dioxane,Water1.2 Reagents: Hydrochloric Acid Solvents: 1,4-Dioxane,Water 标题:Preparation And Application Of The 5-(4-(9-Fluorenylmethyloxycarbonyl)Aminomethyl-3,5-Dimethoxyphenoxy)-Valeric Acid (Pal) Handle For The Solid-Phase Synthesis Of C-Terminal Peptide Amides Under Mild Conditions 作者:Albericio,Fernando; Et Al 参考文献:Journal Of Organic Chemistry 日期:1990 卷标:55(12) 页码:3730-43]
115109-57-4 = 84418-43-9 + 115109-65-4 反应条件:1.1 Reagents: Hydroxyamine Hydrochloride Solvents: Pyridine,Water2.1 Reagents: Hydrogen Catalysts: Palladium Solvents: Acetic Acid,Water3.1 Reagents: Sodium Hydroxide Solvents: 1,4-Dioxane,Water3.2 Reagents: Hydrochloric Acid Solvents: 1,4-Dioxane,Water 标题:Preparation And Application Of The 5-(4-(9-Fluorenylmethyloxycarbonyl)Aminomethyl-3,5-Dimethoxyphenoxy)-Valeric Acid (Pal) Handle For The Solid-Phase Synthesis Of C-Terminal Peptide Amides Under Mild Conditions 作者:Albericio,Fernando; Et Al 参考文献:Journal Of Organic Chemistry 日期:1990 卷标:55(12) 页码:3730-43]
500-99-2 = 84418-43-9 + 115109-65-4 反应条件:1.1 Reagents: Phosphorus Oxychloride2.1 Reagents: Potassium Tert-Butoxide Solvents: Dimethylformamide2.2 Solvents: Dimethylformamide3.1 Reagents: Hydroxyamine Hydrochloride Solvents: Pyridine,Water4.1 Reagents: Hydrogen Catalysts: Palladium Solvents: Acetic Acid,Water5.1 Reagents: Sodium Hydroxide Solvents: 1,4-Dioxane,Water5.2 Reagents: Hydrochloric Acid Solvents: 1,4-Dioxane,Water 标题:Preparation And Application Of The 5-(4-(9-Fluorenylmethyloxycarbonyl)Aminomethyl-3,5-Dimethoxyphenoxy)-Valeric Acid (Pal) Handle For The Solid-Phase Synthesis Of C-Terminal Peptide Amides Under Mild Conditions 作者:Albericio,Fernando; Et Al 参考文献:Journal Of Organic Chemistry 日期:1990 卷标:55(12) 页码:3730-43
((((9H-Fluoren-9-yl)Methoxy)Carbonyl)Amino)Methyl Acetate置于碘代三甲硅烷体系中,化学反应生成 芴甲氧羰酰胺 参考文献:使用三甲基甲硅烷基卤化物活化fmoc保护的n,O-缩醛的机理和合成研究 标题:使用三甲基甲硅烷基卤化物活化fmoc保护的n,O-缩醛的机理和合成研究 摘要:Fmoc保护的n,O-缩醛的三甲基甲硅烷基卤化物活化产生能够有效地添加到多种烯胺中的反应性中间体.NMR研究提供了证据,表明在溶液中形成了稳定的氨基甲酸卤甲基酯中间体.在宽范围的烯胺亲核试剂上都获得了非常好的收率,包括环和非环状的酮衍生和醛衍生的烯胺.初步研究表明,烯胺的添加是通过协调一致的s N 2型机制发生的. DOI:10.1021/ol100494Z
专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
专利号:WO-9837078-A1 优先权日:1997-02-20 标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:WO-9740025-A1 优先权日:1996-04-19 标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA 摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-6515039-B1 优先权日:1998-08-28 标 题:Method for the parallel and combinatory synthesis of compounds bound to a continuous polymeric solid phase supporting material 发明人:ULBRICHT MATHIAS; VOLKMER-ENGERT RUDOLF; GERMEROTH LOTHAR; WENSCHUH HOLGER 权利人:POLY AN GMBH 摘要:The invention relates to a method for the parallel and combinatory synthesis of compounds bound to a continuous polymeric solid phase supporting material. According to the method, a continuous polymeric solid phase supporting material is prepared, the material comprising a matrix of a supporting polymeric material and graft copolymer chains covalently bound to the supporting matrix, the graft copolymer chains having reactive groups being able to react with organic compounds, thereby forming spatially defined reaction sites. The method then comprises the sequential spotting of synthesis building blocks or reagents at the various reaction sites on the continuous solid phase supporting material to yield a substrate library of compounds bound to the solid phase supporting material, whereby each reaction site on the continuous solid phase supporting material determines the composition of the synthesized compound, which is bound directly on the supporting matrix via the reactive groups of the graft polymer chain.
专利号:US-2013267680-A1 优先权日:2010-09-15 标题:Total chemical synthesis of ubiquitin, ubiquitin mutants and derivatives thereof 发明人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL 权利人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL; STICHTING HET NL KANKERINST 摘要:The present invention relates to the field of total chemical synthesis of ubiquitin and related peptides. More in particular, a method is provided of solid phase synthesis of ubiquitin, ubiquitin mutants and derivatives thereof. It was the object of the present invention to provide an approach for the total chemical synthesis of ubuiqitin, which allows for the chemical synthesis of virtually any Ub mutant and giving high overall efficiency and purity. The present inventors have surprisingly found that this object can be realized with a method relying on incorporation of special amino acid building blocks. This approach was found to allow for exceptionally high yields of up to 14% and to provide an synthetic entry into virtually any ubiquitin derivative.
专利号:WO-9817677-A1 优先权日:1996-10-24 标 题 :Improvements in solid-phase synthesis of peptides and related compounds 发明人:ENGLEBRETSEN DARREN 权利人:UNIV QUEENSLAND; ENGLEBRETSEN DARREN 摘要:The invention relates to spacers for use in solid-phase synthesis of peptides and peptide-related compounds, in which a spacer construct is used to ensure that the target peptide or peptide-related compound is at a distance equivalent to at least 5-15 amino acids from the solid support. Constructs of the invention are particularly applicable to the synthesis of strongly hydrophobic peptide, which are otherwise difficult, if not impossible to purify and analyse. The constructs and methods of the invention are also applicable to synthesis of peptide nucleic acids.
[参考文献]: Simon J De Veer, Et Al. Engineered Protease Inhibitors Based On Sunflower Trypsin Inhibitor-1 (Sfti-1) Provide Insights Into The Role Of Sequence And Conformation In Laskowski Mechanism Inhibition. Biochem J. 2015 Jul 15;469(2):243-53.
合成参考文献
参考文献:10.7150/ijms.8.387 摘要:Pipkorn R, Wiessler M, Waldeck W, Lorenz P, Muehlhausen U, Fleischhacker H, Koch M, Braun K. Enhancement of the click chemistry for the inverse Diels Alder technology by functionalization of amide-based monomers. Int J Med Sci. 2011;8(5):387–96.