CAS: 1174018-99-5; (1R,2S,5R)-7-Oxo-2-(Piperidin-4-Ylcarbamoyl)-1,6-Diazabicyclo[3.2.1]Octan-6-Yl Hydrogen Sulfate

上下游产品

Tert-Butyl-4-({[(2S,5R)-7-Oxo-6-(Sulfooxy)-1,6-Diazabicyclo[3.2.1]Oct-2-Yl]Carbonyl}Amino)Piperidine-1-Carboxylate 1174020-65-5
4-[[[(1R,2S,5R)-6-羟基-7-氧代-1,6-二氮杂双环[3.2.1]辛烷-2-基]羰基]氨基]-1-哌啶羧酸叔丁酯 Tert-Butyl 4-((2S,5R)-6-Hydroxy-7-Oxo-1,6-Diazabicyclo[3.2.1]Octane-2-Carboxamido)Piperidine-1-Carboxylate 1174020-64-4
4-[[[(1R,2S,5R)-7-氧代-6-(苯基甲氧基)-1,6-二氮杂双环[3.2.1]辛烷-2-基]羰基]氨基]-1-哌啶羧酸叔丁酯 Tert-Butyl 4-((2S,5R)-6-(Benzyloxy)-7-Oxo-1,6-Diazabicyclo[3.2.1]Octane-2-Carboxamido)Piperidine-1-Carboxylate 1174020-63-3
4-({[(2S,5R)-6-(Benzyloxy)-7-Oxo-1,6-Diazabicyclo[3.2.1]Octan-2-Yl]Carbonyl}Amino)Piperidine-1-Carboxylic Acid Benzyl Ester 1174020-21-3
(2S,5R)-6-(苄氧基)-7-氧代-1,6-二氮杂双环[3.2.1]辛烷-2-羧酸 (2S,5R)-6-(Benzyloxy)-7-Oxo-1,6-Diazabicyclo[3.2.1]Octane-2-Carboxylic Acid 1174020-25-7

1-(2-Nitro)Benzenesulfonyl-(2S,5S)-5-Hydroxypiperidine-2-Carboxylic Acid置于碳酸甲丙酯,4-二甲氨基吡啶,氢气,三氧化硫吡啶,Potassium Carbonate,邻硝基苯磺酰氯,三乙胺,N,N-二异丙基乙胺,Lithium Hydroxide体系中,用 四氢呋喃,甲醇,二氯甲烷,N,N-二甲基乙酰胺,乙酸乙酯,丙酮,乙腈 用作溶剂,-18.0~72.0 °C,411.6 Kpa 条件下,反应 35.85H,反应生成硫酸单[(1R,2S,5R)-7-氧代-2-[(4-哌啶基氨基)羰基]-1,6-二氮杂双环[3.2.1]辛-6-基]酯
参考文献:Practical And Cost-Effective Manufacturing Route For The Synthesis Of A β-Lactamase Inhibitor
标题:Practical And Cost-Effective Manufacturing Route For The Synthesis Of A β-Lactamase Inhibitor
摘要:Compound 1,A Potent And Irreversible Inhibitor Of Beta-Lactamases,Is In Clinical Trials With Beta-Lactam Antibiotics For The Treatment Of Serious And Antibiotic-Resistant Bacterial Infections. A Short,Scalable,And Cost-Effective Route For The Production Of This Densely Functionalized Polycyclic Molecule Is Described.
Doi:10.1021/ol4031606

专利信息

专利号:US-2012053350-A1
优先权日:2009-04-30
标题 :Preparation of alkyl esters of n-protected oxo-azacycloalkylcarboxylic acids
发明人：MANGION IAN; HUFFMAN MARK A; RUCK REBECCA T; LYNCH JOSEPH; CHUNG JOHN Y L; MARCUNE BENJAMIN
权利人:MANGION IAN; HUFFMAN MARK A; RUCK REBECCA T; LYNCH JOSEPH; CHUNG JOHN Y L; MARCUNE BENJAMIN
摘要:A process for the preparation of alkyl esters of N-protected oxo-azacycloalkylcarboxylic acids of Formula III: comprises contacting a ketosulfoxonium ylide of Formula II: with an iridium catalyst to obtain Compound III, wherein P G1 is an amine protective group; k is 0, 1, or 2; and R U , R 1 , R 2 , and R 3 are defined herein. An embodiment of the process further com rises contacting a compound of Formula I: with a sulfoxonium halide of formula (R U ) 3 S(O)Z, wherein Z is halide, in the presence of a strong base to obtain Compound II. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as β-lactamase inhibitors.

专利号:US-9604985-B2
优先权日:2013-06-10
标 题 :Process for the preparation of chiral tert-butyl 4-((1R,2S,5R)-6(benzyloxy)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamido)piperidine-1-carb derivatives and (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide
发明人：MILLER STEVEN P; LIMANTO JOHN; ZHONG YONG-LI; YASUDA NOBUYOSHI; LIU ZHIJIAN
权利人:MERCK SHARP & DOHME
摘要:A process for the preparation of N-protected 6-(piperidin-4-ylcarbamoyl)piperidin-3-yl sulfonates of Formula (III): which comprises contacting a lactone of Formula (II): with an azacycloalkylamine of formula (II-Am): followed by contact with a sulfonyl halide of formula (II-Su): R 4 —SO 2 W (II-Su) in the presence of tertiary amine base, wherein P G1 and P G2 are amine protective groups; k, p and q are 0, 1, or 2, and W, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , and R 9 are defined herein. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as β-lactamase inhibitors.

专利号:US-2023398101-A1
优先权日:2022-06-09
标题 :Co-agents as Therapy Against Anaerobic Pathogens
发明人：PACE JOHN LEE; HARTSELL THERESA LYNN
权利人:FLEURIR ABX LLC
摘要:Co-agent combinations and/or formulations herein unexpectedly display significantly better antimicrobial activity (e.g., more efficacy and/or more potency) against anaerobic pathogens not previously considered targets. With three or more co-agents, selected from a group of a fosfomycin, a diaminopyridine, a sulfonamide, a beta lactam antibacterial, a bacterial beta-lactamase inhibitor, a bacterial fosfomycin-modifying enzyme, and a bacterial peptidoglycan synthesis inhibitor, the therapeutic potential of the three or more co-agents is expanded by targeting a broader spectrum of pathogens. Co-agents, by unexpected synergistic action in an anaerobic environment, are now active and efficacious against difficult to treat pathogenic anaerobes (including anaerobes that cannot utilize oxygen and/or reside in an anaerobic environment, some being inhibited by oxygen), as well as pathogens considered resistant or intolerant to at least one of the co-agents when used singly in an anaerobic environment. Some co-agent combinations and/or formulations contain one or more existing antibiotic agents being repurposed for utility against difficult to treat anaerobic pathogens.

专利号:ES-2921205-T3
优先权日:2017-11-02
标题:Use of statins to overcome resistance to beta-lactam antibiotics in bacterial species that synthesize isoprenoids via the mevalonate synthesis pathway