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バロフロキサシン

バロフロキサシン 化学構造式
127294-70-6
CAS番号.
127294-70-6
化学名:
バロフロキサシン
别名:
バロフロキサシン;バロフロキサシン水和物;バロフロキサシン水和物 (JAN)
英語化学名:
Balofloxacin
英語别名:
q35;BALOFLOXACIN;BALOFLOXACIN 98.5%;Balofloxacin425.46;Balofloxacin, >=99%;Balofloxacin hydrate;Balofloxacin USP/EP/BP;BALOFLOXACIN 98.5% EXTRA PURE;3-quinolinecarboxylicacid,1,4-dihydro-1-cyclopropyl-6-fluoro-8-methoxy-7-(3-(;1-Cyclopropyl-6-fluoro-8-methoxy-7-(3-(methylamino)piperidin-1-yl)-4-oxo-1,4-dihydroquinoline-
CBNumber:
CB0728838
化学式:
C20H24FN3O4
分子量:
389.42
MOL File:
127294-70-6.mol

バロフロキサシン 物理性質

融点 :
137°C
沸点 :
608.3±55.0 °C(Predicted)
比重(密度) :
1.40±0.1 g/cm3(Predicted)
貯蔵温度 :
Keep in dark place,Inert atmosphere,2-8°C
酸解離定数(Pka):
6.44±0.50(Predicted)
外見 :
neat
BRN :
8362117
CAS データベース:
127294-70-6(CAS DataBase Reference)

安全性情報

WGK Germany  3

バロフロキサシン 価格 もっと(6)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01COBQA-7920 バロフロキサシン
Balofloxacin
127294-70-6 1g ¥21600 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01COBQA-7920 バロフロキサシン
Balofloxacin
127294-70-6 5g ¥64800 2021-03-23 購入
林純薬工業株式会社 R125725M ---
Balofloxacin ---
127294-70-6 25mg ¥14500 2021-03-22 購入
富士フイルム和光純薬株式会社(wako) W01FLC223915
1-Cyclopropyl-6-fluoro-8-methoxy-7-(3-(methylamino)piperidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
127294-70-6 5g ¥84400 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01MAS094170
1-Cyclopropyl-6-fluoro-8-methoxy-7-(3-(methylamino)piperidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
127294-70-6 250mg ¥408200 2021-03-23 購入

バロフロキサシン 化学特性,用途語,生産方法

効能

抗菌薬, 核酸合成阻害薬

説明

Balofloxacin, a novel orally-active fluoroquinolone antibiotic, was introduced in South Korea for the treatment of urinary tract infections (UTI). It can be synthetized by reaction of 3-(methylamino)piperidine with the classical 4-quinolone-3-carboxylic acid template. In vitro antibacterial activity of balofloxacin against gram-positive bacteria (Staphylococcus aureus including methicillin-resistant S. aureus, Staphylococcus epidermis, Streptococcus pneumonia, Streptococcus pyrogenes) was almost equal to that of sparfloxacin or tosufloxacin, in contrast its activity against gram-negative bacteria was 2 times or more lower. In clinical trials, balofloxacin was well tolerated and showed comparable efficacy to ofloxacin in patients with UTls. After oral administration, balofloxacin was well absorbed, and was primarily eliminated unchanged in the urine with an elimination half-life of approximately 8 h. In animal studies, balofloxacin did not exhibit any phototoxicity.

化学的特性

Crystalline Solid

Originator

Chugai Pharmaceutical (Japan)

使用

Fluorinated quinolone antibacterial.

使用

Balofloxacin is quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase.

Manufacturing Process

(1) A mixture of ethyl 1-cyclopropyl-6,7,8-trifluoro-1,4-dihydro-4- oxoquinoline-3-carboxylate (933 mg), 3-acetamidopiperidine (710 mg), triethylamine (400 mg) and dimethylsulfoxide (10 ml) was heated at 100°C for 2 hours with stirring. Thereafter the mixture was cooled down and ice water was added thereto. The resulting mixture was extracted with chloroform and the chloroform layer was washed with water three times before being dried over anhydrous sodium sulfate. Removal of the solvent in vacuum followed by purification by silica gel column chromatography (chloroformethanol) gave ethyl 7-(3-acetamidopiperidin-1-yl)-1-cyclopropyl-6,8-difluoro- 1,4-dihydro-4-oxo quinoline-3-carboxylate (930 mg). Re-crystallization from ethanol-ether afforded a colorless crystalline substance (MP: 217°-218°C).
(2) Ethyl 7-(3-acetamidopiperidin-1-yl)-1-cyclopropyl-6,8-difluoro-1,4-dihydro- 4-oxo-quinoline-3-carboxylate obtained from the foregoing step: (a) (433 mg) of above product was dissolved in 6 N hydrochloric acid (5 ml) and heated at 100°C. for 2.5 hours with stirring. After the removal of the solvent in vacuum, methanol was added to the residue and the insoluble materials were filtered off. Removal of the solvent followed by purification by silica gel column chromatography (chloroform-methanol) gave hydrochloride of 7-(3-aminopiperidin-1-yl)-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4- oxoquinoline-3-carboxylic acid (colorless, crystalline-powder). MP: color change at about 272°C, decomposition at about 280°C.
(b) A mixture of 7-(3-acetamidopiperidin-1-yl)-1-cyclopropyl-6,8-difluoro-1,4- dihydro-4-oxoquinoline-3-carboxylic acid (4.05 g), sodium methoxide (2.16 g) and N,N-dimethylformamide (120 ml) was stirred for 2 hours at 100°-140°C. The reaction mixture was concentrated in vacuum and water was added to the residue. The mixture was neutralized with 1 N hydrochloric acid and the neutralized mixture was then concentrated in vacuum. Purification of the concentrated mixture by silica gel column chromatography (chloroformmethanol) gave 7-(3-acetamidopiperidin-1-yl)-1-cyclopropyl-6-fluoro-1,4- dihydro-8-methoxy-4-oxoquinoline-3-carboxylic acid. MP: 248°-250°C.
(c) 7-(3-Acetamidopiperidin-1-yl)-1-cyclopropyl-6-fluoro-1,4-dihydro-8- methoxy-4-oxoquinoline-3-carboxylic acid (1.25 g) above obtained was suspended in 6 N hydrochloric acid (30 ml) and ethanol (5 ml) and heated at 100°C for 3 hours. Then the reaction mixture was concentrated in vacuum and the residue was purified by silica gel column chromatography (chloroform:methanol:ammonium hydroxide=100:30:5) to afford 7-(3- aminopiperidin-1-yl)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4- oxoquinoline-3-carboxylic acid. MP: 176°-177°C.

brand name

Q-Roxin

Therapeutic Function

Antibacterial

応用例(製薬)

A 6-fluoro-8-methoxy quinolone derivative. It has good antistaphylococcal activity (MIC 0.4–4 mg/L), but is inactive against methicillin-resistant Staph. aureus (MRSA) and quinolone-resistant Staph. aureus; Str. pneumoniae is inhibited by 0.4 mg/L. It has good activity against Enterobacteriaceae, but is inactive against Ps. aeruginosa (MIC 8–16 mg/L). After a 200 mg oral dose a peak level of 1.7 mg/L is reached in 1 h. The apparent elimination halflife is about 8 h, rising to 13 h in elderly subjects. Plasma protein binding is about 16%. It was withdrawn from the market in Japan because of adverse events, but is available in China.

バロフロキサシン 上流と下流の製品情報

原材料

準備製品


バロフロキサシン 生産企業

Global( 252)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
Capot Chemical Co.,Ltd.
+86(0)13336195806 +86-571-85586718
+86-571-85864795 sales@capotchem.com China 20012 60
Henan DaKen Chemical CO.,LTD.
+86-371-66670886
info@dakenchem.com China 20907 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22607 55
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29954 58
Shaanxi Yikanglong Biotechnology Co., Ltd.
17791478691
yklbiotech@163.com CHINA 297 58
Shanghai Arbor Chemical Co., Ltd.
021-60451682
021-60451683 act@arborchemical.com CHINA 906 58
Xiamen AmoyChem Co., Ltd
+86 592-605 1114
sales@amoychem.com CHINA 6369 58
Shanghai Longyu Biotechnology Co., Ltd.
+8615821988213
+86 15821988213 info@longyupharma.com China 2473 58
Chongqing Chemdad Co., Ltd
+86-13650506873
sales@chemdad.com CHINA 37282 58
Alchem Pharmtech,Inc.
8485655694
sales@alchempharmtech.com United States 63726 58

127294-70-6(バロフロキサシン)キーワード:


  • 127294-70-6
  • 3-Quinolinecarboxylic acid, 1-cyclopropyl-6-fluoro-1,4-dihydro-8-Methoxy-7-[3-(MethylaMino)-1-piperidinyl]-4-oxo-
  • 1-Cyclopropyl-6-fluoro-8-Methoxy-7-(3-(MethylaMino)piperidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
  • 1-Cyclopropyl-6-fluoro-8-methoxy-7-(3-(methylamino)piperidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-c
  • 1-Cyclopropyl-6-fluoro-8-methoxy-7-(3-(methylamino)piperidin-1-yl)-4-oxo-1,4-dihydroquinoline-
  • Balofloxacin, >=99%
  • 1-cyclopropyl-6-fluoro-1,4- dihydro-8-methoxy-7-(3-methylaminopiperidin-1-yl)-4-oxoquinoline-3-carboxylic acid
  • BALOFLOXACIN
  • 3-quinolinecarboxylicacid,1,4-dihydro-1-cyclopropyl-6-fluoro-8-methoxy-7-(3-(
  • q35
  • BALOFLOXACIN 98.5% EXTRA PURE
  • BALOFLOXACIN 98.5%
  • Balofloxacin 1-cyclopropyl-6-fluoro-1,4- dihydro-8-methoxy-7-(3-methylaminopiperidin-1-yl)-4-oxoquinoline-3 carboxylic acid 1-Cyclopropyl-6-Fluoro-1,4-Dihydro-8-Methoxy-7-[3-(Methylamino)-1-Piperidino]-4-Oxo-3-Quinoline Carboxylic Acid(Balofloxacin)
  • 1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[3-(methylamino)-1-piperidino]-4-oxo-3-quinolinecarboxylicacid
  • (±)-1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[3-(methylamino)piperidino]-4-oxo-3-quinolinecarboxylic Acid
  • 1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[3-(methylamino)-1-piperidinyl]-4-oxo-3-quinolinecarboxylic Acid
  • 1-Cyclopropyl-6-fluoro-8-methoxy-7-(3-methylamino-1-piperidyl)-4-oxo-quinoline-3-carboxylic acid
  • 1-Cyclopropyl-6-fluoro-1,4- dihydro-8-methoxy-7-(3-methylaminopiperidin-1-yl)-4-oxoquinoline-3-carboxylic
  • Balofloxacin hydrate
  • Balofloxacin425.46
  • Balofloxacin USP/EP/BP
  • バロフロキサシン
  • バロフロキサシン水和物
  • バロフロキサシン水和物 (JAN)
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