专利号:US-6218138-B1 优先权日:1998-05-26 标 题 :Synthesis of beta-lactam antibiotics with immobilized penicillin amidase 发明人:ILHAN FERHAT; KRAEMER DIETER 权利人:UNIFAR KIMYA SANAYI VE TICARET 摘要:Beta-lactam antibiotics are synthesized by reacting an amino-beta-lactam component with a corresponding amino-group-containing acylating side-chain component in the presence of penicillin amidase from E. coli covalently immobilized on support particles. The resulting beta-lactam antibiotic product is solubilized by adding an acid such as sulfuric acid to lower the pH to 1.0 at a temperature in the range of 0° C. to +5° C. The immobilized penicillin amidase is substantially inactivated by the acid. After separating the beta-lactam antibiotic product, the immobilized penicillin amidase is substantially reactivated for reuse in antibiotic synthesis by treatment with a buffer having about a neutral pH. Antibiotics that can be produced include ampicillin, amoxicillin, cephalexin, cefaclor and cefadroxil. Support particles that can be used include particles having a macroporous structure and a particle diameter of 10-1000 mum, particles having oxirane groups, particles made of a synthetic polymer and inorganic particles such as porous glass particles.
专利号:US-2018222848-A1 优先权日:2015-08-04 标 题:Salt of Dihydrophenylglycine Methyl Ester 发明人:VAN DER DOES THOMAS; MOODY HAROLD MONRO; LI WEIDONG 权利人:DSM SINOCHEM PHARM NL BV 摘要:The present invention relates to the hemi sulfuric acid salt of methyl (R)-2-amino-2-(cyclohexa-1,4-dien-1-yl)acetate, also trivially referred to as the hemi sulfuric acid salt of D-dihydrophenylglycine methyl ester, to a method for the preparation of said salt and to the use of said salt in the enzymatic synthesis of antibiotics.
专利号:US-8017776-B2 优先权日:2003-07-15 标题 :Methods for synthesis of acyloxyalkyl compounds 发明人:BHAT LAXMINARAYAN; GALLOP MARK A 权利人:XENOPORT INC 摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
专利号:US-4340672-A 优先权日:1979-09-19 标 题:Enzymatic synthesis of β-lactam antibacterials 发明人:KONDO EIJI; MITSUGI TAKASHI; FUJIWARA TAMIO; MUNEYUKI RYONOSUKE 权利人:SHIONOGI & CO 摘要:Penicillins and cephalosporins can be synthesized by the action of an acylase on a penicillin or cephalosporin nucleus amine as substrate and an ester (I) of the following formula as the acyl source: (I) (wherein RCO is an acyl group in penicillin or cephalosporin side chains; X is a hydrogen atom, lower alkyl group or hydroxy-lower alkyl group; Y is a hydrogen atom or a lower alkyl group; and n is a positive integer). The novel acyl source (I) is also disclosed.
专利号:US-9693999-B2 优先权日:2011-01-26 标题:Small molecule RNase inhibitors and methods of use 发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE 权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education 摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.
专利号:US-8143437-B2 优先权日:2002-02-19 标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof 发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X 权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC 摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
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合成参考文献
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