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-2009221834-A1 优先权日:2006-04-20 标题 :Synthesis of 5-Beta-Keto-1,2,4-Oxadiazoles and Conversion of 5-Beta-Keto-1,2,4 Oxadiazoles to N-Pyrazolyl Amidoximes 发明人:JENSEN DAVID R; SIDENSTICK JOHN E 权利人:JENSEN DAVID R; SIDENSTICK JOHN E 摘要:The disclosed invention relates to a process for preparing 5-β-keto-1,2,4-oxadiazoles of formula (I), and conversion of 5-β-keto-1,2,4-oxadiazoles (I) into N-pyrazolyl amidoximes of the formula (II) through reaction with hydrazine. The process is defined by two steps. An amidoxime, which may be prepared in situ, is condensed with a β-keto ester to form a 5-β-keto-1,2,4-oxadiazole. The 5-β-keto-1,2,4-oxadiazole is subsequently reacted with hydrazine to furnish the desired N-pyrazolyl amidoxime. The disclosed invention provides several advantages over the current state of the art for the synthesis of N-pyrazolyl amidoximes, which require the condensation of a pyrzolylamine with an actived substrate and subsequent reaction with hydroxyl amine. N-pyrazolyl amidoximes are useful synthetic intermediates, especially for the preparation of photographic developing chemicals.
专利号:US-2003004337-A1 优先权日:2000-05-04 标 题 :Efficient lactam synthesis 发明人:JUNG KYUNG WOON; YOON CHEOL HWAN 摘要:Lactams, libraries of lactams, and an efficient method of synthesizing a lactam, including a γ-lactam, in which an a-diazoacetamide of the general structure (I) is reacted under conditions promoting intramolecular C-H insertion, for example in the presence of a rhodium salt such as Rh 2 (OAc) 4 , n n n by which means lactams that are precursors in the synthesis of diverse natural and synthetic products, including pyrrolidinone compounds such as lactacystin, pramanicin, kainic acid, statine, AHPPA, and rolipram, are produced.
专利号:US-11807600-B2 优先权日:2021-11-12 标题 :Synthesis of novel ketone body analogs for use as a nutritional supplement 发明人:ROZZONI SAMUEL J; SAUER DARYL R 权利人:ROZZONI SAMUEL J; SAUER DARYL R 摘要:When a healthy and balanced diet is not achieved, nutritional supplements are used to help deal with the resulting health issues and enhance the body's performance. The present invention relates to a novel category of molecules that combine the properties of both ketone bodies and β-Hydroxy β-Methylbutyrate (HMB) that can be used as supplements for treating a wide range of health-related issues. Acetoacetate and β-Hydroxybutrate along with isopentyldiol were used as the sources of ketone bodies and HMB, respectively. The present invention provides a method of synthesis for a new group of compounds that incorporate the properties found in acetoacetate and 3-hydroxybutyrate molecules with that of β-hydroxy β-methylbutyrate.
专利号:US-6689890-B2 优先权日:2000-05-04 标 题:Efficient lactam synthesis 发明人:JUNG KYUNG WOON; YOON CHEOL HWAN 权利人:UNIV SOUTH FLORIDA 摘要:Lactams, libraries of lactams, and an efficient method of synthesizing a lactam, including a gamma-lactam, in which an alpha-diazoacetamide of the general structure (I) is reacted under conditions promoting intramolecular C-H insertion, for example in the presence of a rhodium salt such as Rh2(OAc)4,by which means lactams that are precursors in the synthesis of diverse natural and synthetic products, including pyrrolidinone compounds such as lactacystin, pramanicin, kainic acid, statine, AHPPA, and rolipram, are produced.
专利号:US-5292891-A 优先权日:1991-02-21 标 题 :Optically active 2,2-dimethyl-1,3-dioxin-4-ones and method for preparing same and method for preparing optically active compound for synthesis of physiologically active substance and optically active intermediate compound 发明人:KANEKO CHIKARA; SATO MASAYUKI 权利人:CHISSO CORP 摘要:There are provided novel and optically active 2,2-dimethyl-1,3-dioxin-4-ones which are useful as starting materials for physiologically active compounds, functional materials or the like. Provided are optically active 5,6-epoxyhexanoic acid esters and novel optically active 6-substituted tetrahydropyran-2-one derivatives. That is, optically active 6-chloromethyltetrahydropyran-2-one can be synthesized by lactonizing optically active 2,2-dimethyl-6-(3-chloro-2-hydroxypropyl)-1,3-dioxin-4-one to form optically active 6-chloromethyltetrahydropyran-2,4-dione; reacting the thus formed compound with hydrogen in the presence of a catalyst to obtain optically active 6-chloromethyl-4-hydroxytetrahydropyran-2-one; subjecting this compound to a dehydration reaction, thereby obtaining optically active 6-chloromethyldihydropyran-2-one; reacting this compound with hydrogen in the presence of a catalyst to form optically active 6-chloromethyltetrahydropyran-2-one; and then treating this compound under basic conditions to prepare an optically active 5,6-epoxyhexanoic acid ester represented by the formula (6) ##STR1## (wherein the symbol * represents an asymmetric carbon atom, and R is a methyl group or an ethyl group).
参考标题:Reaction Of α-Oxoketenes With 2-Substituted Benzothiazoles And Benzimidazoles: Synthesis Of Benzo[4,5]Thiazolo[3,2-A]Pyridinone And N-(1,3-Benzothiazol-2-Yl)-3-Oxopropanamide Derivatives 作者:Mahboobeh Zahedifar,Hassan Sheibani |发布日期:2016.1 摘要:Cyclocondensation Reactions Of α-Oxoketenes With 2-Substituted Benzothiazoles Have Been Investigated. Acyl-Substituted Meldrum'S Acids And 1,3-Dioxin-4-One Derivatives Have Been Used As Starting Compounds For Preparation Of α-Oxoketenes, Which Were Used In The Cycloaddition Reactions With (Benzothiazol-2-Yl)-Acetonitrile And (Benzimidazol-2-Yl)Acetonitrile Giving Good Product Yields. Also The Reaction Of (Ch
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