9005-53-2 = 110-17-8 + 141-82-2 + 6915-15-7 + 87-69-4 + 110-16-7 + 144-62-7 + 50-21-5 + 110-15-6 反应条件:1.1R:H2So4,R:H2O2 标题:Electrochemical Conversion Of Lignin To Short-Chain Carboxylic Acids 作者:By Sun,Shirong Et Al 参考文献:Green Chemistry 日期:2023 卷标:25(8) 页码:3127-3136]
9004-34-6 = 110-17-8 + 141-82-2 + 110-16-7 + 144-62-7 + 50-21-5 + 79-14-1 + 110-15-6 反应条件:1.1R:R:O2,S:H2O,175°C,30 Bar 标题:Lignin Alkaline Oxidation Using Reversibly-Soluble Bases 作者:By Kruger,Jacob S. Et Al 参考文献:Green Chemistry 日期:2022 卷标:24(22) 页码:8733-8741]
16133-25-8 = 110-17-8 + 881681-00-1 反应条件:1.1 Reagents: Diisopropylethylamine Catalysts: 4-(Dimethylamino)Pyridine Solvents: 1,4-Dioxane; 0 - 10 °C; < 10 °C2.1 Reagents: Hydrogen Catalysts: Nickel Solvents: Acetic Acid,Tetrahydrofuran,Water3.1 Reagents: Sodium Borohydride Solvents: Methanol3.2 Solvents: Dimethylacetamide 标题:An Efficient,Scalable And Eco-Friendly Synthesis Of 4,5-Substituted Pyrrole-3-Carbonitriles By Intramolecular Annulation On Pd/c And Hzsm-5 作者:Chen,Jianchao; Et Al 参考文献:Chemcatchem 日期:2019 卷标:11(7) 页码:1943-1948]
101953-61-1 = 110-17-8 + 87233-61-2 反应条件:1.1 Reagents: Phosphorus Oxychloride2.1 - 标题:Synthesis Of 2-(4-Substituted-1-Piperazinyl)Benzimidazoles As H1-Antihistaminic Agents 作者:Iemura,Ryuichi; Et Al 参考文献:Journal Of Medicinal Chemistry 日期:1986 卷标:29(7) 页码:1178-83]
57-13-6 = 110-17-8 + 87233-61-2 反应条件:1.1 -2.1 Reagents: Phosphorus Oxychloride3.1 - 标题:Synthesis Of 2-(4-Substituted-1-Piperazinyl)Benzimidazoles As H1-Antihistaminic Agents 作者:Iemura,Ryuichi; Et Al 参考文献:Journal Of Medicinal Chemistry 日期:1986 卷标:29(7) 页码:1178-83]
95893-88-2 = 110-17-8 + 87233-61-2 反应条件:1.1 Reagents: Sodium Hydroxide,Zinc Solvents: Ethanol,Water2.1 -3.1 Reagents: Phosphorus Oxychloride4.1 - 标题:Synthesis Of 2-(4-Substituted-1-Piperazinyl)Benzimidazoles As H1-Antihistaminic Agents 作者:Iemura,Ryuichi; Et Al 参考文献:Journal Of Medicinal Chemistry 日期:1986 卷标:29(7) 页码:1178-83]
110-76-9 = 110-17-8 + 87233-61-2 反应条件:1.1 -2.1 Reagents: Sodium Hydroxide,Zinc Solvents: Ethanol,Water3.1 -4.1 Reagents: Phosphorus Oxychloride5.1 - 标题:Synthesis Of 2-(4-Substituted-1-Piperazinyl)Benzimidazoles As H1-Antihistaminic Agents 作者:Iemura,Ryuichi; Et Al 参考文献:Journal Of Medicinal Chemistry 日期:1986 卷标:29(7) 页码:1178-83]
1807642-39-2 = 110-17-8 + 881681-00-1 反应条件:1.1 Reagents: Hydrogen Catalysts: Nickel Solvents: Acetic Acid,Tetrahydrofuran,Water2.1 Reagents: Sodium Borohydride Solvents: Methanol2.2 Solvents: Dimethylacetamide 标题:An Efficient,Scalable And Eco-Friendly Synthesis Of 4,5-Substituted Pyrrole-3-Carbonitriles By Intramolecular Annulation On Pd/c And Hzsm-5 作者:Chen,Jianchao; Et Al 参考文献:Chemcatchem 日期:2019 卷标:11(7) 页码:1943-1948]
4318-37-0 = 110-17-8 + 87233-61-2 [标题:Reaction Conditions 标题:Synthesis Of 2-(4-Substituted-1-Piperazinyl)Benzimidazoles As H1-Antihistaminic Agents 作者:Iemura,Ryuichi; Et Al 参考文献:Journal Of Medicinal Chemistry 日期:1986 卷标:29(7) 页码:1178-83]
110-16-7 = 110-17-8 反应条件:1.1 Reagents: Acetone; 3 H,25 °C 标题:Microflow Photochemistry - A Reactor Comparison Study Using The Photochemical Synthesis Of Terebic Acid As A Model Reaction 作者:Aida,Shin; Et Al 参考文献:Tetrahedron Letters 日期:2012 卷标:53(42) 页码:5578-5581
专利号:WO-2013138200-A1 优先权日:2012-03-13 标 题 :Green chemistry synthesis of the malaria drug amodiaquine and analogs thereof 发明人:FORTUNAK JOSEPH MARIAN; KULKARNI AMOL ANANT; KING CHRISTOPHER 权利人:UNIV HOWARD 摘要:Methods are provided for a green chemistry one-pot synthesis of amodiaquine and amodiaquine analogs. The methods have a lower environmental impact, lower investment cost, reduced amounts of byproducts and impurities, and a shorter synthesis time, compared to current conventional synthesis methods. The methods reduce the total number of steps in the synthesis from four to five down to two, thereby simplifying production; and allow a reduced number of solvents and reagents to be used in production, thereby reducing the waste generated in the synthesis. The methods can reduce the waste to about 3-5 kilograms of waste generated per kilogram of product produced; and surprisingly improve the overall yield from 60-65% to greater than 90% as compared to the current conventional synthesis methods for amodiaquine and its analogs.
专利号:US-7928223-B2 优先权日:2008-06-20 标题:Process for the synthesis of 7,8-dimethoxy-1,3-dihydro-2H-3-benzazepin-2-one, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:LERESTIF JEAN-MICHEL; LECOUVE JEAN-PIERRE; BRIGOT DANIEL 权利人:SERVIER LAB 摘要:Process for the synthesis of the compound of formula (I): n n n n n n n n n n Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
专利号:US-9193691-B2 优先权日:2012-04-27 标题:Methods for the synthesis of activated ethylfumarates and their use as intermediates 发明人:KRAFT KELLY SULLIVAN; FREEMAN JOHN J; SERWINSKI PAUL; PAVIA VINNIE; PHANSTIEL OTTO; KAUR NAVNEET 权利人:MANNKIND CORP; MANNKIND CORP 摘要:Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4-nitrophenyl, diphenylphosphoryl azide, pivaloyl chloride, chlorosulfonyl isocyanate, p-nitrophenol, MEF, trifluoroacetyl and chlorine, for example, ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl-diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput.
专利号:US-8927708-B2 优先权日:2013-03-26 标 题 :Process for the synthesis of 7,8-dimethoxy-1,3-dihydro-2H-3-benzazepin-2-one compounds, and application in the synthesis of ivabradine 发明人:LE FLOHIC ALEXANDRE 权利人:SERVIER LAB 摘要:Process for the synthesis of the compound of formula (I): n nwherein R represents a para-methoxybenzyl (PMB) group or the following group:n n nApplication in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid.
专利号:US-8779122-B2 优先权日:2012-11-08 标 题:Process for the synthesis of (2E)-3-(3,4-dimethoxyphenyl)prop-2-enenitrile, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:CARRANZA MARIA DEL PILAR; GARCIA ARANDA MARIA ISABEL; GONZALEZ JOSÉ LORENZO; SANCHEZ FRÉDÉRIC 权利人:SERVIER LAB 摘要:Process for the synthesis of the compound of formula (I): n nApplication in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
专利号:US-8426612-B2 优先权日:2009-04-22 标 题:Synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5[2-(phenylsulfonyl)ethyl]-1H-indole 发明人:SERAFINI SIRO; CASTELLIN ANDREA; DAL SANTO CLAUDIO 权利人:SERAFINI SIRO; CASTELLIN ANDREA; DAL SANTO CLAUDIO; ITALIANA SINT SPA 摘要:The present invention refers to the synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole, a drug known by the name Eletriptan, or of its salts. In particular, the present invention regards a process for the synthesis of Eletriptan or of its salt, comprising the following steps: a) Salifying the intermediate of Formula (6), using a dicarboxylic acid to obtain a derived salt; b) Optionally, purifying said raw salt obtained according to step a) by solvent crystallization to obtain a purified salt of the intermediate of Formula (6); c) Converting said salt of the intermediate of formula (6) according to step a) or said purified salt according to step b) into an intermediate of formula (10); d) Converting the intermediate of Formula (10) into Eletriptan or its salt.
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合成参考文献
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