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-11046978-B2 优先权日:2016-03-16 标 题:Synthesis of isoprenoids and derivatives 发明人:GONZALEZ RAMON; CLOMBURG JAMES M; CHEONG SEOKJUNG 权利人:UNIV RICE WILLIAM M 摘要:This disclosure generally relates to the use of enzyme combinations or recombinant microbes comprising same to make isoprenoid precursors, isoprenoids and derivatives thereof including prenylated aromatic compounds. Novel metabolic pathways exploiting Claisen, aldol, and acyioin condensations are used instead of the natural mevalonate (MVA) pathway or 1-deoxy-d-xylulose 5-phosphate (DXP) pathways for generating isoprenoid precursors such as isopentenyl pyrophosphate (IPP), dimethylallyl pyrophosphate (DMAPP), and geranyl pyrophosphate (GPP). These pathways have the potential for better carbon and or energy efficiency than native pathways. Both decarboxylative and non-carboxylative condensations are utilized, enabling product synthesis from a number of different starting compounds. These condensation reactions serve as a platform for the synthesis of isoprenoid precursors when utilized in combination with a variety of metabolic pathways and enzymes for carbon rearrangement and the addition/removal of functional groups. Isoprenoid alcohols are key intermediary products for the production of isoprenoid precursors in these novel synthetic metabolic pathways.
专利号:US-12338202-B2 优先权日:2021-09-10 标 题 :One pot synthesis of urea (meth)acrylates 发明人:BESTGEN SEBASTIAN; BEYER SILVIA 权利人:EVONIK OPERATIONS GMBH 摘要:A one-pot synthesis of polymerizable and acyclic urea (meth)acrylates, preferably mono(meth)acrylates, can be performed via in-situ synthesis of urea alcohols or amines followed by direct reaction with a (meth)acrylate reactive diluent. The urea alcohol/amine is obtained from isocyanates and alcohols, amines, or hydroxyamines. Subsequently, the reaction with the (meth)acrylate reactive diluent takes place and the urea (meth)acrylate is directly obtained either in solution with the reactive diluent, or as a pure material after removal of the reactive diluent.
专利号:US-6252105-B1 优先权日:1998-07-06 标题:Synthesis of low-fluoride organic compounds 发明人:BRAUN MAX; EICHER JOHANNES; JANSSENS FRANCINE; EICHHOLZ KERSTIN; PALSHERM STEFAN 权利人:SOLVAY FLUOR & DERIVATE 摘要:Organic compounds, e.g. fluorinated organic compounds such as fluorinated carboxylic acids or fluorinated carboxylic acid chlorides, may contain small amounts of carboxylic acid fluorides, hydrogen fluoride or hydrolyzable fluoride, which during the preparation of derivatives of the fluorinated organic compounds, for example by esterification, may yield corrosive fluorides or hydrogen fluoride. The invention is a method for the synthesis and/or purification of preferably fluorinated organic compounds such as carboxylic acids, carboxylic acid chlorides and derivatives such as esters thereof, starting from corresponding carboxylic acid chlorides containing acid fluorides or hydrolyzable fluoride, and alcohols under the catalytic action of 'onium' salts of carboxylic acids, to obtain products which have a low fluoride content. Alternatively, an inorganic oxide adsorbent is utilized. The method is especially suitable for the synthesis of esters of trifluoroacetic acid, chlorodifluoroacetic acid, trifluoroacetoacetic acid and/or difluoroacetoacetic acid.
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:WO-03031376-A1 优先权日:2001-10-12 标 题 :Solid phase synthesis of substituted 1,5-benzodiazepine-2-one and 1,5-benzothiazepine-2-one 发明人:MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 权利人:AVENTIS PHARMA INC; MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 摘要:A solid phase synthetic method for making substituted 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one. The method is useful for synthesis of large numbers of compounds through automated parallel synthesis or combinatorial library generation and is thus important to rapid discovery or new therapeutic agents containing the base structure of 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one.
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