专利号:US-11512303-B2 优先权日:2017-05-27 标 题 :Engineered polypeptides and their applications in the synthesis of beta-hydroxy-alpha-amino acids 发明人:CHEN HAIBIN; BONG YONG KOY; XU QING; ZHOU AMENG; SHEN TIANRAN; YANG JIADONG; YANG ZHUHONG 权利人:ENZYMASTER NINGBO BIO ENG CO LTD 摘要:The present invention provides engineered polypeptides that are useful for the asymmetric synthesis of β-hydroxy-α-amino acids under industrial-relevant conditions. The engineered polypeptides disclosed in this invention were developed through directed evolution based on the ability of catalytic synthesis of (2S, 3R)-2-amino-3-hydroxy-3-(4-nitrophenyl) propanoic acid. The present disclosure also provides polynucleotides encoding engineered polypeptides, host cells capable of expressing engineered polypeptides, and methods of producing β-hydroxy-α-amino acids using engineered polypeptides. Compared to other processes of preparation, the use of the engineered polypeptides of the present invention for the preparation of β-hydroxy-α-amino acids results in high purity of the desired stereoisomers, mild reaction conditions, low pollution and low energy consumption. So, it has good industrial application prospects.
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-6121054-A 优先权日:1997-11-19 标 题 :Method for separation of liquid and solid phases for solid phase organic syntheses 发明人:LEBL MICHAL 权利人:TREGA BIOSCIENCES INC 摘要:A simple, efficient apparatus and method for separation of solid and liquid phases useful in methods of high-throughput combinatorial organic synthesis of large libraries or megaarrays of organic compounds is disclosed. The apparatus and method are useful, whether as part of an automated, robotic or manual system for combinatorial organic synthesis. In a preferred embodiment, an apparatus and method of removal of liquid phase from solid phase compatible with microtiter plate type array(s) of reaction vessels is disclosed.
专利号:US-2023183175-A1 优先权日:2020-03-16 标 题:Method for preparing intermediate for use in synthesis of florfenicol and compounds prepared thereby 发明人:LI WENSEN; ZHANG WENQI 权利人:HEADING NANJING PHARMTECHNOLOGIES CO LTD 摘要:The present invention provides a method for preparing an intermediate of florfenicol, comprising: reacting p-methylthiobenzaldehyde with isocyanoacetate under catalysis of a chiral catalyst. In the reaction, the chiral product is oxidized to form a methylsulfone-substituted product which is subsequently deformylized to obtain the intermediate. In the method of the present invention, the chiral center of the intermediate is directly generated in the first step of reaction, and the yield of the first step reaches 75%-80%, which is significantly higher than the conventional chiral resolution methods (about 40% yield), and the product has high chiral purity. The method of the present invention does not use anhydrous copper sulfate that pollutes the environment, which reduces the environmental pressure. The compound of p-methylthiobenzaldehyde and the compound of isocyanoacetate are used to react to form a chiral intermediate, which has higher material availability and efficiency than linear synthesis methods.
专利号:US-5783577-A 优先权日:1995-09-15 标题 :Synthesis of quinazolinone libraries and derivatives thereof 发明人:HOUGHTEN RICHARD A; OSTRESH JOHN M 权利人:TREGA BIOSCIENCES INC 摘要:The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.
专利号:US-6025526-A 优先权日:1999-02-10 标 题 :Synthesis of substituted mercapto-benzaldehydes 发明人:SOROKIN VIKTOR D; FERTEL LAWRENCE B 权利人:OCCIDENTAL CHEM CO 摘要:Disclosed is a composition of (1) a substituted benzaldehyde having the general formula ##STR1## where X is a leaving group in the ortho or para position, (2) a mercaptide having the general formula MSR' in an amount about stoichiometric to about 20 mole % in excess of stoichiometric with the amount of said substituted benzaldehyde, where M is an alkali metal and R' is alkyl or haloalkyl from C 1 to C 8 or aryl, aralkyl, or alkyl from C 6 to C 12 , (3) sufficient water to dissolve said mercaptide and MX, (4) about 0.1 to about 5 mole %, based on said substituted benzaldehyde, of a phase transfer catalyst, and (5) 0 to about 100 wt %, based on total composition weight, of a water-immiscible organic solvent. Heating the composition to a temperature between about room temperature and 100° C. results in the formation of a substituted mercapto-benzaldehyde.
[参考文献]: Matthias Onghena, Et Al. Development And Application Of A Non-Targeted Extraction Method For The Analysis Of Migrating Compounds From Plastic Baby Bottles By Gc-Ms. Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2014;31(12):2090-102.
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