CAS: 3511-16-8; Hetacillin

上下游产品

hetacillin 6-epi-ampicillin 2-(3,6-dioxo-5-phenylpiperazine-2-yl)-5,5-dimethylthiazolidine-4-carboxylic acid hetacillin methyl ester hetacillin methyl ester S-oxide

📜Hetacillin 在 Sodium Hydroxide体系中,反应 1.0H,以92%的收率获得6-Epi-Hetacillin
参考文献:Chemical Reactivity Of Penicillins And Cephalosporins. Intramolecular Involvement Of The Acyl-Amido Side Chain
标题:Chemical Reactivity Of Penicillins And Cephalosporins. Intramolecular Involvement Of The Acyl-Amido Side Chain
摘要:The Rate Of Degradation Of B-Epi-Ampicillin In Acidic,Neutral,And Alkaline Aqueous Solutions Was Followed At 35 Degrees C And An Ionic Strength Of 0.5 Mol Dm(-3) (Kcl) By High-Performance Liquid Chromatography (Hplc) And Spectrophotometric Assays. Pseudo-First-Order Rate Constants Were Determined In A Variety Of Buffer Solutions,And The Overall Ph-Rate Profile Was Obtained By Extrapolation To Zero Buffer Concentration. The Hydrolysis Of 6-Epi-Ampicillin Is Subject To Acid And Hydroxide-Ion Catalysis And,For A Penicillin,An Unusual Ph-Independent Reaction. Intramolecular General Base-Catalyzed Hydrolysis By The Side Chain Amido Group Is Proposed To Explain The Enhanced Rate Of Neutral Hydrolysis Of 6-Epi-Ampicillin And Cephalosporins. The Beta-Lactam Of 6-Epi-Ampicillin Also Undergoes Intramolecular Aminolysis By Nucleophilic Attack Of The 6-Alpha Side Chain Amino Group To Give A Stable Piperazine-2,5-Dione Derivative. The Low Effective Molarity For Intramolecular Aminolysis Of Only 40 M Is Partly Attributed To The Unfavorable Trans To Cis Isomerization About The B-Amide Side Chain Required For Ring Closure. Theoretical Calculations Show That The Intramolecular Aminolysis Of 6-Epi-Ampicillin Nucleophilic Attack ocurs From The Alpha-Face Of The Beta-Lactam Ring With An Activation Energy Of 14.4 Kcal/Mol.
Doi:10.1021/Jo981628J

专利信息

专利号:US-2005186197-A1
优先权日:2002-08-29
标 题:Peptide inhibitors of beta lactamases
发明人：PALZKILL TIMOTHY; HUANG WANZHI
摘要:Peptide inhibitors of β-lactamases have been identified by the synthesis of peptide arrays using synthesis SPOT technology. These peptide inhibitors of β-lactamase have activity against a broad spectrum of β-lactamases and are useful in a variety of applications.

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-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.

专利号:EP-0024372-A1
优先权日:1979-08-03
标题:Derivatives of clavulanic acid, their preparation and pharmaceutical compositions containing them
发明人：DENERLEY PAUL MILLINGTON; EGLINGTON ALFRED JOHN; HARBRIDGE JOHN BARRY
权利人:BEECHAM GROUP PLC
摘要:The compounds of the formula (II):n and salts and esters thereof wherein the hydroxyl group occupies position 2 or 4 R 1 and R 2 may be the same or different and represent hydrogen, halogen, hydroxy, lower alkyl, cyclopentyl, cyclohexyl, lower alkoxy or R, and R 2 when an adjacent carbon atoms may together represent a 1,4-buta-1,3-dienylene group or a polymethylene group containing from 3 to 5 carbon atoms; have been found to be β-lactam antibiotics and synergists with penicillins and cephalosporins. Their preparation and use is described. The synthesis of intermediates useful in their preparation is also described.

专利号:WO-9925385-A1
优先权日:1997-11-17
标 题:A method of increasing nucleic acid synthesis with ultrasound
发明人：UNGER EVAN C; MCCREERY THOMAS; SADEWASSER DAVID
权利人:IMARX PHARMACEUTICAL CORP
摘要:The present invention is directed to a method of increasing nucleic acid synthesis in a cell comprising administering to the cell a therapeutically effective amount of ultrasound for a therapeutically effective time such that said administration of said ultrasound results in said increased nucleic acid synthesis. The nucleic acid sequence may comprise an endogenous sequence or an exogenous sequence.