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Balofloxacin

Product Name
Balofloxacin
CAS No.
127294-70-6
Chemical Name
Balofloxacin
Synonyms
q35;BALOFLOXACIN;Barlow of sand;BALOFLOXACIN 98.5%;Balofloxacin425.46;Balofloxacin, >=99%;Balofloxacin hydrate;Balofloxacin USP/EP/BP;Cypermethrin Impurity 4;BALOFLOXACIN 98.5% EXTRA PURE
CBNumber
CB0728838
Molecular Formula
C20H24FN3O4
Formula Weight
389.42
MOL File
127294-70-6.mol
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Balofloxacin Property

Melting point:
137°C
Boiling point:
608.3±55.0 °C(Predicted)
Density 
1.40±0.1 g/cm3(Predicted)
storage temp. 
Keep in dark place,Inert atmosphere,2-8°C
solubility 
H2O : < 0.1 mg/mL (insoluble)DMSO : 0.67 mg/mL (1.72 mM; Need ultrasonic)
pka
6.44±0.50(Predicted)
form 
Solid
color 
White to off-white
BRN 
8362117
CAS DataBase Reference
127294-70-6(CAS DataBase Reference)
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H228Flammable solid

Precautionary statements

P403Store in a well-ventilated place.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
25504
Product name
Balofloxacin
Purity
≥98%
Packaging
500mg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
25504
Product name
Balofloxacin
Purity
≥98%
Packaging
1g
Price
$62
Updated
2024/03/01
Cayman Chemical
Product number
25504
Product name
Balofloxacin
Purity
≥98%
Packaging
5g
Price
$266
Updated
2024/03/01
Cayman Chemical
Product number
25504
Product name
Balofloxacin
Purity
≥98%
Packaging
10g
Price
$458
Updated
2024/03/01
Usbiological
Product number
264273
Product name
Balofloxacin
Packaging
250mg
Price
$233
Updated
2021/12/16
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Balofloxacin Chemical Properties,Usage,Production

Description

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.

Chemical Properties

Crystalline Solid

Originator

Chugai Pharmaceutical (Japan)

Uses

Fluorinated quinolone antibacterial.

Uses

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

Pharmaceutical Applications

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.

Balofloxacin Preparation Products And Raw materials

Raw materials

Preparation Products

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Balofloxacin Suppliers

Jiangyin Yongda Chemical Co., Ltd
Tel
0519-85777058
Fax
+86-510-86652688, 86656628
Email
info@yongdachina.com
Country
China
ProdList
74
Advantage
78
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
ZHIWE CHEMTECH CO LTD
Tel
021-20221225 13917446399
Fax
QQ:115820162
Email
sales@zhiwe.net
Country
China
ProdList
604
Advantage
61
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
19172
Advantage
64
XiaoGan ShenYuan ChemPharm co,ltd
Tel
15527768850
Email
1791901229@qq.com
Country
China
ProdList
8844
Advantage
52
China Langchem Inc.
Tel
0086-21-58956006
Fax
0086-21-58956100
Country
China
ProdList
7811
Advantage
57
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
Country
China
ProdList
4727
Advantage
58
ShangHai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847 13636370518
Fax
021-55068248
Email
shyysw007@163.com
Country
China
ProdList
4940
Advantage
60
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View Lastest Price from Balofloxacin manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
Balofloxacin 127294-70-6
Price
US $0.00/KG
Min. Order
1KG
Purity
98.0%
Supply Ability
500kg/month
Release date
2021-07-01
Hangzhou Hyper Chemicals Limited
Product
Balofloxacin 127294-70-6
Price
US $0.00-0.00/KG
Min. Order
1KG
Purity
USP, BP
Supply Ability
5,000KG
Release date
2024-06-13
Hebei Chuanghai Biotechnology Co,.LTD
Product
Balofloxacin 127294-70-6
Price
US $1.90/KG
Min. Order
1KG
Purity
99%
Supply Ability
10 ton
Release date
2024-08-15

127294-70-6, BalofloxacinRelated Search:


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  • C20H24FN3O4
  • C20H24FN3O42H2O
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Antibacterial
  • White crystal powder