Sodium; 6-[2-((E)-2-ethoxycarbonyl-1-methyl-vinylamino)-2-(4-hydroxy-phenyl)-acetylamino]-3,3-dimethyl-7-oxo-4-thia-1-aza-bicyclo[3.2.0]heptane-2-carboxylatepenicillin G
合成工艺路线路线简述
,,阿莫西林,,盐酸置于ice,Sodium Hydroxide体系中,化学反应 2.0H,反应生成 阿莫西林三水合物 参考文献:Silylation Process 标题:Silylation Process 摘要:一种将6-氨基青霉烷酸或7-氨基脱乙酰基头孢菌素酸硅化的方法,该方法是在某些羧酸酯中进行硅化,并且可用于生产6-α-氨基酰基青霉素和7-α-氨基酰基脱乙酰基头孢菌素.
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-4251442-A 优先权日:1978-12-07 标题:Method for synthesis of penicillin 发明人:MORITA YOSHIHARU; ITAGAKI TAKAHARU; ITO TSUYOSHI; WADA SHIGENORI 权利人:MITSUBISHI CHEM IND 摘要:This invention relates to a method for synthesizing a penicillin by reacting a silylate of 6-aminopenicillanic acid and a carboxylic acid halide in the presence of an insoluble weakly basic resin having a three-dimensional structure.
专利号:WO-2014128538-A1 优先权日:2013-02-22 标 题:A process for the preparation of amoxicillin trihydrate 发明人:GUJRAL RAJINDER SINGH 权利人:VARDHMAN CHEMTECH LTD; GUJRAL RAJINDER SINGH 摘要:The invention relates to an in-situ process for the preparation of amoxicillin trihydrate from sugarcane juice without isolation of the intermediates produced during the reaction sequence viz penicillin G and 6-aminopenicillanic acid. The invention provides an in-situ cost effective and environment friendly process in which no separate synthesis of the intermediates, no purification cost and no crystallization cost for the intermediates is required.
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:US-7442386-B2 优先权日:2001-08-16 标题:Synthesis and use of reagents for improved DNA lipofection and/or slow release prodrug and drug therapies 发明人:DIAMOND SCOTT L; GRUNEICH JEFFREY ALAN 权利人:UNIV PENNSYLVANIA 摘要:The invention relates to compositions and methods for a one-step synthetic technique for making cationic steroid or cationic drug molecules for use as delivery vehicles. The invention further relates to methods for using cationic steroid molecules in lipofection or transfection, delivery of drugs, and for treatment of inflammation and other diseases and disorders. The invention also relates to cationic steroid prodrugs and cationic prodrugs and to methods of modifying drugs.
专利号:US-9839642-B2 优先权日:2014-05-09 标 题:Beta-tetrazolyl-propionic acids as metallo-beta-lactamase inhibitors 发明人:TANG HAIFENG; YANG SHU-WEI; MANDAL MIHIR; SU JING; LI GUOQING; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; PAN JIANPING; HAGMANN WILLIAM; DING FA-XIANG; XIAO LI; PASTERNAK ALEXANDER; HUANG YUHUA; DONG SHUZHI; YANG DEXI 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
1: Scheinfeld N. A review and report of blistering distal dactylitis due to Staphylococcus aureus in two HIV-positive men. Dermatol Online J. 2007 May 1;13(2):8. Review. Review. Review. Review. Review. Review.
合成参考文献
摘要:S104 | UKVETMED | UK Veterinary Medicines Directorate's List | DOI:10.5281/zenodo.7802119 摘要:Kiso to Rinsho. Clinical Report., 7(3040), 1973