CAS: 41906-86-9; Nitrocefin

化学文摘社编号为41906-869-9,用于化学数据库和监管环境中的精确识别.总的来说,硝氏素在理解和抗击病原细菌抗药性方面发挥着关键作用.

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欧盟法规

ECHA物质C&L通报

上下游产品

Diphenylmethyl 7β-(2-Thienylacetamido)-3-(Hydroxymethyl)-Cephem-4-Carboxylate 29126-13-4
(6R,7R)-4-Methoxybenzyl-3-(Chloromethyl)-8-Oxo-7-(2-(Thiophen-2-yl)Acetamido)-5-Thia-1-Azabicyclo[4.2.0]Oct-2-Ene-2-Carboxylate 101182-25-6
(6R)-3-Bromomethyl-8-Oxo-7T-(2-Thiophen-2-Yl-Acetylamino)-(6Rh)-5-Thia-1-Aza-Bicyclo[4.2.0]Oct-2-Ene-2-Carboxylic Acid Benzhydryl Ester 30361-56-9
7-氨基头孢烷酸 7-Aminocephalosporanic Acid 957-68-6
羟甲基-7-氨基头孢烷酸 D-7-Aca 15690-38-7

合成工艺路线路线简述

  • 合成目标产物 Nitrocefin 主要起始原料 2-Thiopheneacetyl Chloride
  • (文献来源)合成步骤主要原料 2-Thiopheneacetyl Chloride
7-氨基头孢烷酸置于水,三溴化磷,Sodium Carbonate,苯甲醚,三氟乙酸,Sodium Hydroxide体系中,用 四氢呋喃,甲醇,二氯甲烷,水,乙酸乙酯,丙酮 作为反应溶剂,化学反应 18.5H,反应生成 头孢硝噻吩
参考文献:头孢硝噻吩的合成方法
标题:头孢硝噻吩的合成方法
摘要:本发明涉及一种头孢硝噻吩的合成方法,属于药物合成领域.本发明提供了一个全新的以化合物i为原料制备头孢硝噻吩的工艺路线.化合物i可利用7‑aca制得.本发明所用制备方法可以7‑aca为起始原料经七步制得头孢硝噻吩.起始原料7‑aca是头孢菌素关键性中间体,且早已产业化,市场价格低廉.本发明操作简单,反应易处理,产物易纯化,收率高,易于工业化,降低了生产成本.

海关参考信息

专利信息


专利号:EP-1525305-B1
优先权日:2002-08-02
标题:Methods and compositions for in vitro synthesis of proteins in a cell-free system enriched with atp-sulfurylase
发明人:RYABOVA LYUBOV; MASSON JEAN-MICHEL
权利人:PROTEUS
摘要:The present invention provides methods and composition for enhancing in vitro synthesis of biological macromolecules in a cell-free system where ATP is required as a primary energy source, wherein said cell-free system is enriched with ATP-sulfurylase The invention relates also to as cell-free systems and cell-free extracts enriched with ATP-sulfurylase for enhancing in vitro synthesis of any biological macromolecules.

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-2013316397-A1
优先权日:2012-04-30
标 题:Cell-Free Polypeptide Synthesis
发明人:AIREN ISOKEN; SWARTZ JAMES ROBERT
权利人:UNIV LELAND STANFORD JUNIOR
摘要:Methods, microbial strains and reaction mixtures for cell-free synthesis of polypeptides are provided. The methods of the invention utilize a reaction mixture comprising microbial cell extracts that are modified in the protein component relative to an extract from a native cell. The modification may be one or both of (i) increased levels of proteins that increase synthetic yield; and (ii) decreased levels of proteins that decrease synthetic yield. The modification may result from a genetic modification of the microbial cell, or from ex vivo supplementation or depletion of an extract.

专利号:US-2006178357-A1
优先权日:2005-02-10
标题 :Chphalosporin-derived mercaptans as inhibitors of serine and metallo-beta-lactamases
发明人:BUYNAK JOHN D; CHEN HANSONG
权利人:BUYNAK JOHN D; CHEN HANSONG
摘要:Compounds of formula I: See Formula I in Figures Section n nwherein R 1 , R 2 , R 3 , R 4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting simultaneously serine and metallo-β-lactamase enzymes, for enhancing the activity of β-lactam antibiotics, and for treating β-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.

专利号:US-7022691-B2
优先权日:2002-04-04
标题 :Inhibitors of serine and metallo-β-lactamases
发明人:BUYNAK JOHN D; CHEN HANSONG
权利人:BUYNAK JOHN D; CHEN HANSONG
摘要:Compounds of formula (I): n nwherein R 1 , R 2 , R 3 , R 4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting simultaneously serine and metallo-β-lactamase enzymes, for enhancing the activity of β-lactam antibiotics, and for treating β-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.

专利号:US-7125986-B2
优先权日:1997-12-29
标题:Penicillanic acid derivative compounds and methods of making
发明人:BUYNAK JOHN D; RAO AKIREDDY SRINIVASA; DOPPALAPUDI VENKATA RAMANA
权利人:UNIV SOUTHERN METHODIST
摘要:Compounds of formula I: n nwherein R 1 , R 2 , R 3 , R 4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting β-lactamase enzymes, for enhancing the activity of β-lactam antibiotics, and for treating β-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.
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主要参考文献


1: Boehle KE, Gilliand J, Wheeldon CR, Holder A, Adkins JA, Geiss BJ, Ryan EP, Henry CS. Utilizing Paper-Based Devices for Antimicrobial Resistant Bacteria Detection. Angew Chem Int Ed Engl. 2017 May 5. doi: 10.1002/anie.201702776. [Epub ahead of print] doi: 10.1093/jac/dkw521. pii: e02234-16. doi: 10.1128/AAC.02234-16. Print 2017 Mar.
6: Ourghanlian C, Soroka D, Arthur M. Inhibition by Avibactam and Clavulanate of the β-Lactamases KPC-2 and CTX-M-15 Harboring the Substitution N(132)G in the Conserved SDN Motif. Antimicrob Agents Chemother. 2017 Feb 23;61(3). pii: e02510-16. doi: 10.1128/AAC.02510-16. Print 2017 Mar.
7: Kim MK, An YJ, Na JH, Seol JH, Ryu JY, Lee JW, Kang LW, Chung KM, Lee JH, Moon JH, Lee JS, Cha SS. Structural and mechanistic insights into the inhibition of class C β-lactamases through the adenylylation of the nucleophilic serine. J Antimicrob Chemother. 2017 Mar 1;72(3):735-743. doi: 10.1093/jac/dkw491. doi: 10.1016/j.watres.2016.11.066. Epub 2016 Dec 1. doi: 10.1016/j.ijmyco.2016.06.010. Epub 2016 Jun 30. doi: 10.1128/JCM.02092-16. Epub 2016 Dec 7.

合成参考文献


参考文献:10.1128/aac.40.9.2075
摘要:Roychoudhury S, Kaiser RE, Brems DN, Yeh WK. Specific interaction between beta-lactams and soluble penicillin-binding protein 2a from methicillin-resistant Staphylococcus aureus: development of a chromogenic assay. Antimicrob Agents Chemother. 1996 Sep;40(9):2075–9.
摘要:Yang ZC, Yang XS, Wang BC, Sun QY. [Structure-activity relationships of salicylic acid and its analogs in the inhibitory action on beta-lactamase]. Yao Xue Xue Bao. 2006 Mar;41(3):230–2.
参考文献:10.1128/aac.01025-07
摘要:Marchiaro P, Tomatis PE, Mussi MA, Pasteran F, Viale AM, Limansky AS, Vila AJ. Biochemical characterization of metallo-beta-lactamase VIM-11 from a Pseudomonas aeruginosa clinical strain. Antimicrob Agents Chemother. 2008 Jun;52(6):2250–2.
参考文献:10.1021/jm301490d
摘要:Winkler ML, Rodkey EA, Taracila MA, Drawz SM, Bethel CR, Papp-Wallace KM, Smith KM, Xu Y, Dwulit-Smith JR, Romagnoli C, Caselli E, Prati F, van den Akker F, Bonomo RA. Design and exploration of novel boronic acid inhibitors reveals important interactions with a clavulanic acid-resistant sulfhydryl-variable (SHV) β-lactamase. J Med Chem. 2013 Feb 14;56(3):1084–97.
参考文献:10.1002/bit.20202
摘要:Ni Y, Chen RR. Accelerating whole-cell biocatalysis by reducing outer membrane permeability barrier. Biotechnol Bioeng. 2004 Sep 20;87(6):804–11. doi: 10.1002/bit.20202.
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