101799-75-1Relevant academic research and scientific papers
Chlorination at the 8-position of a functionalized quinolone and the synthesis of quinolone antibiotic ABT-492
Barnes, David M.,Christesen, Alan C.,Engstrom, Kenneth M.,Haight, Anthony R.,Hsu, Margaret C.,Lee, Elaine C.,Peterson, Matthew J.,Plata, Daniel J.,Raje, Prasad S.,Stoner, Eric J.,Tedrow, Jason S.,Wagaw, Seble
, p. 803 - 807 (2006)
The total synthesis of quinolone antibiotic ABT-492 has been achieved in 67% yield over nine steps from 2,4,5-trifluorobenzoic acid. The highlights of this synthesis include a novel chemoselective chlorination at the 8-position of a highly elaborated quinolone core. In addition, a Lewis acid promoted cyclization reaction to form the quinolone heterocycle was developed which was incorporated into a one-pot, three-step cyclization/coupling/protection sequence that proceeds in 93% yield.
Syntheses of new pyridonecarboxylic acid derivatives containing 3-, 5- or 6-quinolyl substituents at N-1 and their anti-HIV-RT activities
Oh, Yoon-Seok,Lee, Chi-Woo,Chung, Yong-Ho,Yoon, Sung-June,Cho, Sung-Hye
, p. 541 - 550 (1998)
A series of new pyridonecarboxylic acid derivatives containing 3-, 5- or 6-quinolyl substituents at N-1 were synthesized and their in vitro anti-HIV- RT activities were evaluated. Several compounds in this series showed better activity than Atevirdine.
Probing structural requirements for human topoisomerase I inhibition by a novel N1-Biphenyl fluoroquinolone
Delgado, Justine L.,Lentz, Sarah R.C.,Kulkarni, Chaitanya A.,Chheda, Pratik R.,Held, Hailey A.,Hiasa, Hiroshi,Kerns, Robert J.
, p. 109 - 130 (2019)
Fluoroquinolones substituted with N-1 biphenyl and napthyl groups were discovered to act as catalytically inhibitors of human topoisomerases I and II, and to possess anti-proliferative activity in vivo. Structural requirements for these novel quinolones t
Synthesis of the quinolone ABT-492: Crystallizations for optimal processing
Haight, Anthony R.,Ariman, Sema Z.,Barnes, David M.,Benz, Nancy J.,Gueffier, Francoix X.,Henry, Rodger F.,Hsu, Margaret C.,Lee, Elaine C.,Morin, Larry,Pearl, Kurt B.,Peterson, Matthew J.,Plata, Daniel J.,Willcox, David R.
, p. 751 - 756 (2006)
ABT-492 has been under development at Abbott Laboratories as a quinolone antibiotic. A convergent syntheses was utilized to prepare the compound on a multi-kilogram scale. Difficulties in isolation of intermediates were overcome by developing control of t
Syntheses of new pyridonecarboxylic acid derivatives containing 1- or 2- naphthyl substituents at N-1 and their anti-HIV-RT activities
Oh,Cho
, p. 17 - 23 (1998)
A series of new pyridonecarboxylic acid derivatives containing 1- or 2- naphthyl substituents at N-1 were synthesized at their in vitro anti-HIV-RT activities were evaluated. Several compounds in this series showed better activity than Atevirdine.
Refining method of ciprofloxacin and meglumine hydrochloride thereof
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, (2021/10/27)
The invention provides a preparation process of ciprofloxacin and meglumine thereof. The intermediate product DLSX07 is stirred at Branson ° C. 20% minutes and then sonicated until the solution is cloudy, stirred at room temperature for a period 30s, stirred at room temperature 3h, cooled and slowly added to distilled water, and filtered through suction filtration and filter cake vacuum drying to obtain a pale yellow powder, and 4% the KOH mixture is subjected to ultrasonic treatment 40 - 50 °C. 1. The process is performed by stirring 5h. NCS .t. The solution is cloudy. LC-MS / MS detection powder is deltafloxacin, distilled water is added, and meglumine is mixed to obtain a deltafloxacin meglumine salt. By optimizing the preparation process, the use of the organic solvent is reduced, the reaction time is shortened, and the ice bath and the addition of the interface carrier material contribute to the improvement of the yield.
A kind of improved [...] preparation method (by machine translation)
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Paragraph 0036, (2018/03/24)
The invention belongs to the field of medical synthesis, in particular to a kind of improved [...] preparation method. The technology of this invention can avoid a 4 - benzopyran [...] formation of impurities, and follow-up substituted, cyclized, butt joi
Preparation of deller floxacin and intermediate thereof
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Paragraph 0027; 0033; 0051-0053, (2018/05/30)
The invention relates to preparation of deller floxacin and an intermediate thereof. According to the preparation method of the deller floxacin, the purity of an intermediate compound, a compound A-3and a compound W-4 is limited to be more than 99.0 perce
QUINOLONE-BASED COMPOUNDS WITH ANTICANCER ACTIVITY
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Paragraph 0087, (2018/06/30)
Embodiments are directed to compounds of the formulae (I), (Ia), (Ib), (II), (IIa) (III), (IV), (V), and (VI); methods for treating cancer with one or more compounds of the formulae (I), (Ia), (Ib), (II), (IIa); (III), (IV), (V), and (VI); and methods for
Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety
Liu, Hongmin,Huang, Ju,Wang, Jiayang,Wang, Minghua,Liu, Mingliang,Wang, Bin,Guo, Huiyuan,Lu, Yu
, p. 628 - 638 (2015/01/16)
A series of novel 1-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives 9aed containing an oxime functional moiety were synthesized and evaluated for their biological activity. Our results reveal that 9a1 and 9b3 have good in vitro activity against MTB H37Rv ATCC 27294 (MIC: 0.25 mg/mL) and two MDR-MTB clinical isolates (MICs: 0.065-0.125 mg/mL). Most of 9aed show potent activity against Escherichia coli and Klebsiella pneumoniae (MICs: 50s: 11.43-26.04 mg/kg).
