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-3887606-A 优先权日:1971-06-02 标题 :Process for the preparation of DL-phenylglycine esters 发明人:PHILLIPPS GORDON HANLEY; STEPHENSON LESLIE; COOKSEY ALBERT ROY; CLARK JOHN COLIN 权利人:GLAXO LAB LTD 摘要:A process for the resolution of DL-phenylglycine esters in which said ester is treated with (+)-tartaric acid in the presence of a mixture of solvents of different polarities, one of which is an alkanol having 1-4 carbon atoms, and the (+)-hermitartrate of the D-phenylglycine ester is selectively crystallised therefrom. Dphenylglycine and/or its salts may be obtained by hydrolysis of the ester thus formed. D-phenylglycine is a valuable intermediate in the synthesis of antibiotics of the penicillin and cephalosporin types. The present invention provides a relatively cheap, high yield process for the production of optically active esters of phenylglycine by way of their diastereoisomeric salts and for the production of optically active phenylglycine therefrom. Novel D-phenylglycine esters and salts are disclosed.
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-3759898-A 优先权日:1971-09-14 标 题 :Synthesis of alpha-(carbo(5-indanyloxy)) benzylpenicillin 发明人:NAKANISHI S 权利人:PFIZER 摘要:THE PREPARATION OF A-(CARBO(5-INDANYLOXY))BENZYLPENICILLIN VIA THE ESTERIFICATION OF A-CARBOXYPENICILLIN WITH 5-INDANOL IN THE PRESENCE OF N, N''-DICYCLOHEXYLCARBODIIMIDE IN A REACTION-INERT SOLVENT AT A PH OF 2-8.
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.
1: Tune BM, Fravert D, Hsu CY. Oxidative and mitochondrial toxic effects of cephalosporin antibiotics in the kidney. A comparative study of cephaloridine and cephaloglycin. Biochem Pharmacol. 1989 Mar 1;38(5):795-802. 8: Barbhaiya RH, Turner P. Fluorimetric assay of cephradine, cephalexin and cephaloglycin. Br J Clin Pharmacol. 1977 Aug;4(4):427-31. 9: Tune BM, Fravert D. Mechanisms of cephalosporin nephrotoxicity: a comparison of cephaloridine and cephaloglycin. Kidney Int. 1980 Nov;18(5):591-600.
合成参考文献
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