专利号:US-11059835-B2 优先权日:2014-08-15 标 题 :Synthesis of cephalosporin compounds 发明人:WALLER DAVID; GAZDA GREGORY; MINDEN ZACHARY; BARTON LISA; LEIGH CLIFTON 权利人:MERCK SHARP & DOHME 摘要:Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction.
专利号:US-10941161-B2 优先权日:2014-08-15 标 题:Intermediates in the synthesis of cephalosporin compounds 发明人:MOSHOS KRISTOS ADRIAN; JURKAUSKAS VALDAS; FOGLIATO GIOVANNI; SCANU MANUEL; HWANG YOU SEOK 权利人:MERCK SHARP & DOHME 摘要:Described herein are crystalline forms of a compound of formula (III′), including toluene solvates of TATD-CLE, as well as processes for the preparation thereof and use thereof in the preparation of cephalosporin compounds such as ceftolozane.
专利号:US-9695196-B2 优先权日:2014-06-20 标 题 :Reactions of thiadiazolyl-oximinoacetic acid derivative compounds 发明人:MOSHOS KRISTOS ADRIAN; JURKAUSKAS VALDAS; SCANU MANUEL; BENOTTI MICHELE 权利人:MERCK SHARP & DOHME 摘要:This disclosure relates to an improved synthesis of cephalosporin antibiotic compounds such as ceftolozane, and compositions and methods of use thereof. Thiadiazolyl-oximinoacetic acid compounds such as TATD can be reacted to yield the activated thiadiazolyl-oximinoacetic acid methanesulfonate ester compounds useful in the manufacture of cephalosporin antibiotic compounds.
专利号:US-2019225624-A1 优先权日:2014-08-15 标题:Intermediates in the synthesis of cephalosporin compounds
专利号:EP-3180347-B1 优先权日:2014-08-15 标 题:Synthesis of cephalosporin compounds
专利号:US-2018170949-A1 优先权日:2014-12-30 标 题 :Synthesis of cephalosporin compounds
1: Eckmann C, Solomkin J. Ceftolozane/tazobactam for the treatment of complicated intra-abdominal infections. Expert Opin Pharmacother. 2015 Feb;16(2):271-80. doi: 10.1517/14656566.2015.994504. Epub 2014 Dec 22. 3: Chandorkar G, Xiao A, Mouksassi MS, Hershberger E, Krishna G. Population pharmacokinetics of ceftolozane/tazobactam in healthy volunteers, subjects with varying degrees of renal function and patients with bacterial infections. J Clin Pharmacol. 2015 Feb;55(2):230-9. doi: 10.1002/jcph.395. Epub 2014 Nov 14. 4: Estabrook M, Bussell B, Clugston SL, Bush K. In vitro activity of ceftolozane-tazobactam as determined by broth dilution and agar diffusion assays against recent U.S. Escherichia coli isolates from 2010 to 2011 carrying CTX-M-type extended-spectrum β-lactamases. J Clin Microbiol. 2014 Nov;52(11):4049-52. doi: 10.1128/JCM.02357-14. Epub 2014 Aug 20.
合成参考文献
参考文献:10.1021/acs.jmedchem.4c00983 摘要:Kawai A, Yamasaki K, Otagiri M, Doi Y. Interaction of Cephalosporins with Human Serum Albumin: A Structural Study. J. Med. Chem. 2024 Jul 31;67(16):14175–83. doi: 10.1021/acs.jmedchem.4c00983.