专利号:US-9388131-B2 优先权日:2011-04-27 标题:Automated synthesis of small molecules using chiral, non-racemic boronates 发明人:BURKE MARTIN D; LI JUNQI; GILLIS ERIC P 权利人:UNIV ILLINOIS 摘要:Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.
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:WO-2015120485-A1 优先权日:2014-02-10 标 题:Water, bubble collapse and syngas species in the synthesis of graphene and its derivatives 发明人:SHANKMAN RICHARD S 权利人:PEERLESS WORLDWIDE LLC 摘要:Hydrodynamic cavitation-inducing inertial, non-inertial, and combination reactors are employed in the hydrothermal synthesis of graphene and its derivatives, both in solution and vapor. Various hydrodynamic cavitation reactor embodiments are revealed. Water is used to both nucleate and 'self-heal' graphene sheet growth in solution and vapor. Various methods of combustion, hydrothermal and dehydration synthesis of graphene and its derivatives are revealed. Additionally, water and ice are used as a substrate, both alone and in combination with other substrates, to grow and recover useful graphene and its derivatives.
专利号:WO-03050105-A2 优先权日:2001-12-10 标题 :Catalytic asymmetric synthesis of optically active compounds 发明人:HALLAND NIS; JOERGENSEN KARL ANKER; HANSEN TORE 权利人:CHEMINOVA AS; HALLAND NIS; JOERGENSEN KARL ANKER; HANSEN TORE 摘要:A one step catalytic asymmetric process for the synthesis of an optically active compound of formula la or lb wherein R is selected from C1-7 alkyl, C1-7 haloalkyl, C1-7 alkoxy, C1-7 haloalkoxy, halogen and hydroxy; R3 is H or C1-4 alkyl; R4 is selected from H, C1-7 alkyl, C1-7 haloalkyl, C1-7 alkoxy, COOH, CO-C1-7 alkoxy and an optionally substituted aryl or heterocycle; AR represents C1-7 alkyl, optionally substituted aryl, an optionally substituted heterocycle or AR and R4 may be bridged together forming part of a ring system; X is O or S; m is a number between 0-4; comprising the step of reacting a compound of the formula 2 with a compound of formula 3 in the presence of a catalytic amount of a chiral nitrogen containing organic compound.
专利号:US-7964743-B2 优先权日:2005-02-17 标 题:Catalyst for asymmetric synthesis, ligand for use therein, and process for producing optically active compound through asymmetric synthesis reaction using them 发明人:MIYAURA NORIO; YAMAMOTO YASUNORI 权利人:JAPAN SCIENCE & TECH AGENCY 摘要:Compounds represented by the following general formula (1a) or (1b). n nA complex comprising a center metal of rhodium and a compound represented by the following general formula (1a) or (1b) as a ligand. A catalyst for optically active beta-substituted carbonyl compound synthesis and catalyst for asymmetric 1, 2 addition reaction being composed of the complex. A method of production of an optically active beta-aryl compound from an alpha, beta-unsaturated compound and an aryl-boronic acid derivative and method of production of an optically active aryl alcohol compound from an aldehyde compound and aryl boronic acid derivatives using the catalyst. A complex comprising a center metal of palladium and a compound represented by the following general formula (1a) or (1b) as a ligand. A catalyst for asymmetric allylic substitution reaction being composed of the complex. A method of production of an optically active dialkyl (1,3-disubstituted propeny)malonate compound from a 1,3-disubstituted ally acetate compound and a dialkyl malonate and method of production of an optically active allylamine compound from a 1,3-disubstituted ally acetate compound and an amine compound. The compounds have not only the versatility of being usable in the synthesis of wide-ranging optically active aryl compounds but also the selectivity and reactivity permitting synthesis with high yield within a short period of time under industrially advantageous mild conditions.
专利号:US-6799120-B2 优先权日:2000-02-03 标 题:Nonredundant split/pool synthesis of combinatorial libraries 发明人:SEPETOV NIKOLAI F; ISSAKOVA OLGA L; BAUM STEPHEN A; OSTREM JAMES A 权利人:NANOSCALE COMBINATORIAL SYNTHE 摘要:The present invention includes methods for generating combinatorial libraries on solid phase supports in which increased productivity is achieved by pooling all common steps in synthesis without using a tracking or coding system to record the synthetic history of each compound. Methods for generating combinatorial libraries in which containers with random mixtures of solid phase particles are divided and combined together in non-random ways without the exchange of particles between containers are also provided. Various products are optionally produced in multi-stage syntheses according to the invention, such as oligomers and synthetic non-repetitive organic molecules. The methods additionally relate to the identification of each library component without adding extra synthetic, physical, optical, or electronic encoding steps during library synthesis. Combinatorial synthetic systems are also provided.
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合成参考文献
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