专利号:EP-0454867-B1 优先权日:1989-11-17 标题:A METHOD FOR THE SYNTHESIS OF $g(a), $g(b)-UNSATURATED KETONES 发明人:TSUKASHIMA KEIICHI TAKAOKA PLA; NAKAJIMA MASASHI TAKAOKA PLANT; FUJIMARU MASAYOSHI TAKAOKA PLA; SUZUKI KENJI TAKAOKA PLANT 权利人:NIPPON SODA CO 摘要:The present invention relates to a method for the synthesis of alpha , beta -unsaturated ketones which comprises, in the method for the synthesis of alpha , beta -unsaturated ketones represented by general formula (I) (where R<1> is an aliphatic group with a side chain at the 1 position, an alicyclic group, a substituted alicyclic group, a heterocyclic group, a substituted heterocyclic group, a phenyl group or a substituted phenyl group), reacting aldehydes represented by general formula (II): R<1>CHO (where R<1> is as defined above) with alkali metal salt of acetoacetic acid represented by general formula (III) (where M<+> is an alkali metal ion), in the presence as a catalyst of 3-azabicyclo[3,2,2] nonane, a cyclic secondary amine represented by general formula (1) (where n is 3 or more and up to 5, m is 1 or more and up to 10, R<2> is an alkyl group having 1 to 10 carbon atoms and of straight chain or with side chains, an alkyl group substituted by alicyclic groups or phenyl groups, an alicyclic group which may be substituted by lower alkyl groups, or a phenyl group which may be substituted by lower alkyl groups, and an R<2> substitution position is at a carbon atom other than the two adjacent to N), a cyclic secondary amine represented by general formula (2) (where l is 1 or more and up to 6, a ring with N is a 6-membered, 7-membered or 8-membered ring, the two neighbors of N are methylene, R<3> is a lower alkyl group, its substitution position is at a carbon atom other than the two adjacent to N, and (a) is an alicyclic group or a phenyl group), or a secondary amine represented by general formula (3): CH3NHCH2R<4> (where R<4> is an aliphatic group having 5 to 17 carbon atoms and of straight chain or with side chains, an alicyclic group which may be substituted by lower alkyl groups, a phenyl group which may be substituted by lower alkyl groups, or an alkyl group substituted by phenyl groups), in a mixture solvent of water and water-insoluble organic solvent, while keeping the pH constant with mineral acid, and by adjusting the amount of water.
专利号:US-5484949-A 优先权日:1993-01-29 标题:Method for the synthesis of α β-unsaturated ketones 发明人:TSUKASHIMA KEIICHI; NAKAJIMA MASASHI; FUJIMARU MASAYOSHI; SUZUKI KENJI 权利人:NIPPON SODA CO 摘要:The present invention relates to a method for the synthesis of alpha , beta -unsaturated ketones which comprises, in the method for the synthesis of alpha , beta -unsaturated ketones represented by general formula reacting aldehydes represented by general formula R1CHO (where R1 is as defined above) with alkali metal salt of acetoacetic acid represented by general formula sence as a catalyst of 3-azabicyclo[3,2,2]nonane, a cyclic secondary amine represented by general formula (1) (1) a cyclic secondary amine represented by general formula (2) (2) (where, l is 1 or more and up to 6, a ring with N is a 6-membered, 7-membered or 8-membered ring, the two neighbors of N are methylene, R3 is a lower alkyl group, its substitution position is at a carbon atom other than two those adjacent to N, and is an alicyclic group or a phenol group), or a secondary amine represented by general formula (3) CH3NHCH2R4(3) in a mixuture solvent of water and water-insoluble organic solvent, while keeping the pH constant with mineral acid, and by adjusting an amount of water.
专利号:US-2005014954-A1 优先权日:2001-11-22 标 题:Pyrrole synthesis 发明人:OHRLEIN REINHOLD; BAISCH GABRIELE 摘要:The invention relates to a novel process for the preparation of N-substituted pyrroles, especially of formula (V), wherein the radicals are as defined in the description, by intermolecular aza-Wittig reaction starting from organic azides and 1,4-dioxo compounds. The invention relates also to novel iminophosphorane intermediates for this synthesis. The resulting pyrroles are useful, for example, in the organic synthesis of pharmaceuticals or other active substances and chemicals.
专利号:US-9982005-B2 优先权日:2013-04-04 标 题 :Macrolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.
专利号:US-7399773-B2 优先权日:2001-01-09 标 题 :Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid and phenylamide 发明人:NELSON JADE DOUGLAS; PAMMENT MICHAEL GERARD 权利人:WARNER LAMBERT CO 摘要:An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide by a novel synthesis is described where methyl cyanoacetate is converted in eight operations or fewer to the desired product, as well as other valuable intermediates used in the process.
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.
参考标题:A General Proline‐catalyzed Synthesis Of 4,5‐disubstituted N ‐sulfonyl‐1,2,3‐triazoles From 1,3‐dicarbonyl Compounds And Sulfonyl Azide 作者:Shanmugam Rajasekar,Pazhamalai Anbarasan |发布日期:2019.12.13 摘要:An Efficient Proline-Catalyzed Synthesis Of 4,5-Disubstituted-N-Sulfonyl-1,2,3-Triazoles Has Been Accomplished From 1,3-Dicarbonyl Compounds And Sulfonyl Azides. The Developed Reaction Is Suitable For Various Symmetrical And Unsymmetrical 1,3-Dicarbonyl Compounds, Tolerates Various Functional Groups And Affords 4,5-Disubstituted-N-Sulfonyl-1,2,3-Triazoles In Good Yield With Excellent Regioselectivity
合成参考文献
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