CAS: 25953-19-9; Cefazolin

上下游产品

Delta-3 Methyl Ester Of Cefazolin 79239-19-3
7-氨基-3-{[(5-甲基-1,3,4-噻二唑-2-基)硫]甲基}头孢霉素烷酸 (6R,7R)-7-Amino-3-(5-Methyl-1,3,4-Thiadiazol-2-Ylthiomethyl)-8-Oxo-5-Thia-1-Azabicyclo[4.2.0]Oct-2-Ene-2-Carboxylic Acid 30246-33-4
3-(乙酰氧基甲基)-8-氧代-7-[[2-(四唑-1-基)乙酰基]氨基]-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸 7-((Tetrazol-1'-yl)Acetylamino)-3-Acetyloxymethyl-8-Oxo-5-Thia-1-Azabicyclo[4.2.0]Oct-2-Ene-2-Carboxylic Acid 32510-61-5
头孢菌素 C Cephalosporin C 61-24-5
7-氨基-3-甲基-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-甲酸 3-Deacetyloxy-7-Aminocephalosporanic Acid 22252-43-3
7-氨基头孢烷酸 7-Aminocephalosporanic Acid 957-68-6

头孢菌素 C置于phosphate Buffer,Enzyme Derivative Dao,Enzyme Derivative Ga,Pga E. Coli A体系中,化学反应 5.0H,反应生成头孢唑啉
参考文献:One-Pot Chemoenzymatic Synthesis Of 3'-Functionalized Cephalosporines (Cefazolin) By Three Consecutive Biotransformations In Fully Aqueous Medium
标题:One-Pot Chemoenzymatic Synthesis Of 3'-Functionalized Cephalosporines (Cefazolin) By Three Consecutive Biotransformations In Fully Aqueous Medium
摘要:We Illustrate A New Chemoenzymatic Synthesis Of Cefazolin From Cephalosporin C,Involving Three Consecutive Biotransformations In Full Aqueous Medium. This One-Pot Three-Step Synthesis Includes The D-Amino Acid Oxidase Catalyzed Oxidative Deamination Of The Cephalosporin C Side Chain,Hydrolysis Of The Resulting Glutaryl Derivative Catalyzed By Glutaryl Acylase,And The Final Penicillin G Acylase (Pga)-Catalyzed Acylation Of 7-Aminocephalosporanic Acid (1,7-Aca). The Product,7-[(1H-Tetrazol-1-yl)Acetamido]-3-(Acetoxymethyl)-Delta(3)-Cephem-4-Carboxylic Acid (5),Was Used As An Intermediate For Cefazolin Synthesis By 3'-Acetoxy Group Displacement With 2-Mercapto-5-Methyl-1,3,4-Thiadiazole. Very High Yields Have Been Achieved With All The Enzymatic Reactions Performed; High Product Concentrations Were Obtained In Short Reaction Times. This Synthetic Approach Presents Several Advantages When Compared With The Conventional Chemical Processes. The Use Of The Toxic Reagents And Chlorinated Solvents Is Avoided,While The Substrate Specificity And Chemoselectivity Of The Enzymes Makes Reactive Group Protection And Intermediate Purification Unnecessary. The Enzymatic Deacylation Of Cephalosporin C Was Performed By The Simultaneous Use Of D-Amino Acid Oxidase And Glutaryl Acylase. The Substrate Specificity Of Pga Allowed The Acylation Of 7-Aca (1) To Be Performed Without Purification From The Glutaric Acid Produced During The Enzymatic Deacylation. These Results Were Achieved By Optimization And Correct Assembly Of The Different Biotransformations Involved. Special Attention Has Been Applied To The Kinetically Controlled Acylation Reaction. High Yields Were Obtained Through A Careful Selection Of The Enzyme Catalyst,Experimental Conditions,And Synthetic Strategy.
Doi:10.1021/jo971166U

专利信息

专利号:WO-2024262578-A1
优先权日:2023-06-23
标 题 :Synthesis of cefazolin under sequential continuous-flow conditions
发明人：KOBAYASHI SHU; ISHITANI HARURO; SUGITA SHOICHI
权利人:UNIV TOKYO
摘要:The present disclosure relates to a sequential continuous-flow synthesis of cefazolin, which is a vital first-choice drug used for the prevention of primary infection in most surgeries, was investigated. Rapid flow and efficient mixing of substrates in suitable flow reactors enabled the target compound to be obtained in a short period without any intermediate isolation. A flexible system design that can be applied from a small-scale to medium-scale synthesis could be demonstrated, and optimal parameters were established to realize the synthesis. A 0.3 mol/h scale synthesis was achieved in 54% isolated yield with 13.75 g/h dL space-time-yield of cefazolin. The obtained material had an acceptable impurity profile and could be purified by simple acid-base extraction and precipitation.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:EP-2173892-B8
优先权日:2007-07-27
标题:Process for the preparation of immobilised recombinant Penicillin Acylase biocatalyst from Achromobacter sp CCM 4824 expressed in E. coli BL21 CCM 7394 and its use for the synthesis of beta-lactam antiobiotics
发明人：DATLA ANUPAMA; RAJASEKAR VYASARAYANI WILLIAMS; KYSLIK PAVEL; BECKA STANISLAV; KRISHNAKANT ASHAR TRUPTI; YOGESH ZAMBRE SUJATA; NIKUNJ KUMAR
权利人:FERMENTA BIOTECH LTD
摘要:The present invention discloses isolation of Penicillin Acylase (PA) from Achromobacter sp CCM 4824 expressed in recombinant strain E. coli BL21 CCM 7394 bearing the recombinant plasmid pKXIP1 and processing of PA into biocatalyst useful for the industrial synthesis of antibiotics. More particularly the invention discloses a synthesis of semi-synthetic β-lactam antibiotics in the reaction mixture consisting of activated acyl-donor (D-p-hydroxyphenylglycine methyl ester or amide for Amoxicillin and Cefadroxil; D-phenylglycine methyl ester or amide for Ampicillin and Cephalexin) and nucleophile (6-APA or 7-ADCA) catalyzed by PA obtained from recombinant E. coli BL21 CCM 7394 as the biocatalyst.

专利号:US-2024197774-A1
优先权日:2021-04-16
标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles
发明人：LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO
权利人:UNIV TEXAS
摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.

专利号:US-12221452-B2
优先权日:2017-10-04
标题:Synthesis of cantharidin
发明人：DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
权利人:VERRICA PHARMACEUTICALS INC
摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).

专利号:US-2007015260-A1
优先权日:2002-03-14
标 题:Synthesis of synthons for the manufacture of bioactive compounds
发明人：WONG CHI-HUEY; LIU JUNJIE; DESANTIS GRACE; BURK MARK
权利人:SCRIPPS RESEARCH INST
摘要:The present invention is based on the discovery that 2-deoxyribose-5-phosphate aldolase (DERA, EC 4.1.2.4) and variants thereof can be used to catalyze sequential asymmetric aldol reactions between a wide variety of donor and acceptor aldehydes. The reaction products typically contain at least two new stereogenic centers and can be produced in enantiomerically pure form. As such, DERA catalyzed asymmetric aldol chemistry can be exploited to produce synthons for the synthesis of a variety of bioactive molecules.