CAS: 77912-79-9; Sulfazecin Free Acid

该化合物是主要用于兽医的磺酰胺抗生素,属于硫化物类药物,其特征为磺酰胺功能组,硫化物通过抑制细菌叶酸合成,对细菌生长和繁殖至关重要,从而表现出抗菌性特性;该化合物通常对一系列克型阳性和克-阴性细菌有效;就物理特性而言,硫化物通常作为晶体固体呈色,其溶性因所用溶剂而异;必须指出,硫化素与其他磺酰胺一样,可能会引起某些人的过敏反应,并可能导致诸如皮肤皮疹或胃肠紊乱等不利影响;由于其特定用途和潜在副作用,硫化素在兽医监督下使用,在食品生产动物中使用时须遵守规章准则,以确保食品供应的安全.

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MSDS等安全信息

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      专利信息


      专利号:US-4502994-A
      优先权日:1982-12-09
      标题 :Enantiomeric synthesis of 3-amino-4-carbamoyloxymethyl-2-azetidonone-1-sulfate
      发明人:WEI CHUNG-CHEN; WEIGELE MANFRED
      权利人:HOFFMANN LA ROCHE
      摘要:A novel enantiomeric synthesis from ascorbic acid of (3S,4S)-3-amino-4-carbamoyloxymethyl-2-azetidinone-1-sulfate, an intermediate for an antibiotic compound.

      专利号:US-4461726-A
      优先权日:1982-05-17
      标题 :Desulfurization of penicillins to prepare azetidinones
      发明人:WEI CHUNG-CHEN; WEIGELE MANFRED
      权利人:HOFFMANN LA ROCHE
      摘要:A process for the Raney nickel desulfurization of penicillins is described. In the process of the invention, amino penicillanic acid or derivatives thereof are reacted with Raney nickel under controlled conditions of temperature and time to yield azetidinones which are useful as intermediates for the synthesis of monocyclic beta-lactam antibiotics.

      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.

      专利号:US-4734495-A
      优先权日:1985-07-17
      标 题 :Process and intermediates for beta-lactam antibiotics
      发明人:EVANS DAVID A; SJOGREN ERIC B
      权利人:HARVARD COLLEGE
      摘要:1-Benzyl(or substituted benzyl)-3β-[4(S)-aryloxazolidin-2-one-3-yl]-4β-(2-arylvinyl)azetidin-2-ones are provided via cycloaddition of a 4(S)-aryloxazolidin-2-one-3-ylacetyl halide and an imine formed with a benzylamine and a 3-arylacrolein, e.g. cinnamaldehyde. The azetidinones are useful chiral intermediates in an asymmetric synthesis of 1-carba(1-dethia)-3-hydroxy-3-cephem-4-carboxylic acids and esters and to monocyclic β-lactam antibiotics.

      专利号:US-4870169-A
      优先权日:1985-07-17
      标 题:Intermediates for beta-lactam antibiotics
      发明人:EVANS DAVID A; SJOGREN ERIC B
      权利人:HARVARD COLLEGE
      摘要:1-Benzyl(or substituted benzyl)-3β-[4(S)-aryloxazolidin-2-one-3-yl]-4β-(2-arylvinyl)azetidin-2-ones are provided via cycloaddition of a 4(S)-aryloxazolidin-2-one-3-ylacetyl halide and an imine formed with a benzylamine and a 3-arylacrolein, e.g. cinnamaldehyde. The azetidinones are useful chiral intermediates in an asymmetric synthesis of 1-carba(1-dethia)-3-hydroxy-3-cephem-4-carboxylic acids and esters and to monocyclic β-lactam antibiotics.

      专利号:CN-102126999-B
      优先权日:2010-01-20
      标题 :Method for catalytic synthesis of chiral azetidin-2-one-4-amide and carboxylic acid compounds by microbial system

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      ✅ COA系统入驻 | 共享模式

      主要参考文献


      1: Oliver RA, Li R, Townsend CA. Monobactam formation in sulfazecin by a nonribosomal peptide synthetase thioesterase. Nat Chem Biol. 2018 Jan;14(1):5-7. doi: 10.1038/nchembio.2526. Epub 2017 Nov 20.
      2: Horsman ME, Marous DR, Li R, Oliver RA, Byun B, Emrich SJ, Boggess B, Townsend CA, Mobashery S. Whole-Genome Shotgun Sequencing of Two β-Proteobacterial Species in Search of the Bulgecin Biosynthetic Cluster. ACS Chem Biol. 2017 Oct 20;12(10):2552-2557. doi: 10.1021/acschembio.7b00687. Epub 2017 Sep 26.
      3: Braga D, Lackner G. One Ring to Fight Them All: The Sulfazecin Story. Cell Chem Biol. 2017 Jan 19;24(1):1-2. doi: 10.1016/j.chembiol.2017.01.001. doi: 10.1016/j.chembiol.2016.11.010. Epub 2016 Dec 22.

      合成参考文献


      摘要:S6 | ITNANTIBIOTIC | Antibiotic List from the ITN MSCA ANSWER | DOI:10.5281/zenodo.2621956
      摘要:Nature., 289(590), 1981 []
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