CAS: 163253-35-8; 7-((S)-7-Amino-5-Azaspiro[2.4]Heptan-5-yl)-8-Chloro-6-Fluoro-1-((1R,2S)-2-Fluorocyclopropyl)-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid Sesquihydrate

该化合物是一种复杂的有机化合物,具有独特的结构特征.该物质含有一种碱性核心,这是一种双循环结构,因其生物活动而闻名于此,特别是在医药化学领域.多种功能团体的存在,包括氨基化合物组,一种碳球酸和卤素次成分(氯和氟基),表明它与生物目标之间可能发生相互作用,从而引起对药物开发的兴趣.这种循环结构有助于其三维相融合,从而影响其药理特性.此外,水合形式表明该化合物可与水分子联系在一起,从而影响其溶性和稳定性.

结构式图片

合成工艺路线路线简述

    专利信息


    专利号:US-9353057-B2
    优先权日:2003-12-30
    标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
    发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
    权利人:XENOPORT INC
    摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

    专利号:US-2018148745-A1
    优先权日:2015-05-26
    标题:Hemoprotein catalysts for improved enantioselective enzymatic synthesis of ticagrelor
    发明人:ARNOLD FRANCIS H; RENATA HANS; MCINTOSH JOHN A; LEWIS RUSSELL D; KAN SEK BIK JENNIFER; HERNANDEZ KARI; COELHO PEDRO; ROZZELL DAVID; ZHANG CHEN
    权利人:CALIFORNIA INST OF TECHN; PROVIVI INC
    摘要:The present invention provides methods by which trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine and related cyclopropane compounds are prepared using synthetic strategies that include a biocatalytic cyclopropanation step.

    专利号:US-8093381-B2
    优先权日:2007-05-24
    标题:Method of synthesis of fluoroquinolones
    发明人:BERTHON-CEDILLE LAURENCE; LEGUERN MARIE-EMMANUELLE; RENAUD GILLES; TOMBRET FRANCIS
    权利人:BERTHON-CEDILLE LAURENCE; LEGUERN MARIE-EMMANUELLE; RENAUD GILLES; TOMBRET FRANCIS; BIOCODEX
    摘要:The invention relates to a method of preparation of fluoroquinolones of formula (I) from compounds of formula (II): n nin which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and X are as defined in Claim 1.

    专利号:US-2015158809-A9
    优先权日:2013-02-26
    标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
    发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
    权利人:XENOPORT INC
    摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

    专利号:US-7632944-B2
    优先权日:2007-01-24
    标题 :Quinolone carboxylic acids, derivatives thereof, and methods of making and using same
    发明人:HARMS ARTHUR E
    权利人:BAUSCH & LOMB
    摘要:A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.

    专利号:US-8227597-B2
    优先权日:2006-10-06
    标题 :Quinolone carboxylic acids, derivatives thereof, and methods of making and using same
    发明人:HARMS ARTHUR E
    权利人:HARMS ARTHUR E; BAUSCH & LOMB
    摘要:A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens.
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    1: Wang H, Lekkala S, Ren Y, Tay AJH, Neighbors J, Ebetino FH, Sun S, Joseph NM, Schwarz EM, Xie C. Effects of hydroxybisphosphonates-conjugated sitafloxacin on fracture healing and skeletal growth in mice. JBMR Plus. 2025 Dec 24;10(2):ziaf195. doi: 10.1093/jbmrpl/ziaf195.
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    3: Urabe N, Sakamoto S, Tokita N, Kanokogi T, Tsunehara R, Kishi K. Clinical efficacy of sitafloxacin-containing regimens for Mycobacterium avium complex pulmonary disease. BMC Pulm Med. 2025 Nov 18;25(1):532. doi: 10.1186/s12890-025-04004-1.
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