113028-17-4

• 

• Basic information

  1. Product Name: Ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piprazinyl)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate
  2. Synonyms: 6-FLUORO-1-METHYL-4-OXO-7-(1-PIPERAZINYL)-4H-(1,3)THIAZETO(3,2-A)QUINOLINE-3-CARBOYLIC ACID ETHYL ESTER;6-FLUORO-1-METHYL-4-OXO-7-(1-PIPRAZINYL)-1H,4H-(1,3)THIAZETO(3,2-A)QUINOLINE-3-CARBOXYLIC ACID, ETHYL ESTER;6-Fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H,4H-[1,3]-thiazeto[3,2-a]-3-quinolinecarboxylic acid ethyl ester;ETHYL 6-FLUORO-1-METHYL-4-OXO-7-(1-PIPERAZINYL)-4H-(1,3)-THIAZETO(3,2-A) QUINOLINE-3-CARBOXYLATE;Prulifloxacin Intermediate PL-10;Ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piprazinyl)-4H-(1,3)-thiazeto(3,2-a);Ethyl 6-fluoro-1-Methyl-4-oxo-7-(1-piprazinyl)-4H-;1,6-diMethyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazetidino[3,2-a]quinoline-3-carboxylic acid hydrofluoride
  3. CAS NO:113028-17-4
  4. Molecular Formula: C₁₈H₂₀FN₃O₃S
  5. Molecular Weight: 377.43
  6. EINECS: -0
  7. Product Categories: API intermediates;PRULIFLOXACIN;Other Products
  8. Mol File: 113028-17-4.mol
  9. Article Data: 6

• Chemical Properties

  1. Melting Point: 224 °C
  2. Boiling Point: 579.122 °C at 760 mmHg
  3. Flash Point: 304.042 °C
  4. Appearance: /
  5. Density: 1.441 g/cm³
  6. Vapor Pressure: 0mmHg at 25°C
  7. Refractive Index: 1.679
  8. Storage Temp.: under inert gas (nitrogen or Argon) at 2–8 °C
  9. Solubility: N/A
  10. PKA: 8.69±0.10(Predicted)
  11. CAS DataBase Reference: Ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piprazinyl)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate(CAS DataBase Reference)
  12. NIST Chemistry Reference: Ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piprazinyl)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate(113028-17-4)
  13. EPA Substance Registry System: Ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piprazinyl)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate(113028-17-4)

• Safety Data

  1. Hazard Codes: N/A
  2. Statements: N/A
  3. Safety Statements: N/A
  4. WGK Germany:
  5. RTECS:
  6. HazardClass: N/A
  7. PackingGroup: N/A
  8. Hazardous Substances Data: 113028-17-4(Hazardous Substances Data)

• Suppliers
• Usage
• SDS
• Synthetic route
• Upstream product
• Downstream Products
• Article

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• Ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piprazinyl)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate

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113028-17-4 Usage

General Description

Ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piprazinyl)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate is a chemical compound with a complex molecular structure. It features a thiazetoquinoline core with a fluorine substitution at the 6 position, a methyl group at the 1 position, and a carboxylic ester functional group at the 3 position. Additionally, it contains a piprazinyl group at the 7 position. Ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piprazinyl)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate may have potential pharmaceutical applications, as the quinoline and thiazole moieties are common in a variety of biologically active molecules. However, further research and testing would be necessary to determine its specific properties and potential uses.

Check Digit Verification of cas no

The CAS Registry Mumber 113028-17-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,1,3,0,2 and 8 respectively; the second part has 2 digits, 1 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 113028-17:
(8*1)+(7*1)+(6*3)+(5*0)+(4*2)+(3*8)+(2*1)+(1*7)=74
74 % 10 = 4
So 113028-17-4 is a valid CAS Registry Number.

InChI:InChI=1/C17H18FN3O3S/c1-2-24-17(23)14-15(22)10-7-11(18)13(20-5-3-19-4-6-20)8-12(10)21-9-25-16(14)21/h7-8,19H,2-6,9H2,1H3

113028-17-4SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 17, 2017

Revision Date: Aug 17, 2017

1.Identification

1.1 GHS Product identifier

Product name	Ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piprazinyl)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate

1.2 Other means of identification

Product number	-
Other names	ulifloxacin ethyl ester

1.3 Recommended use of the chemical and restrictions on use

Identified uses	For industry use only.
Uses advised against	no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number	-
Service hours	Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:113028-17-4 SDS

113028-17-4Synthetic route

110-85-0

piperazine

113046-72-3

ethyl 6,7-difluoro-1-methyl-4-oxo-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate

113028-17-4

ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate

Conditions

Conditions	Yield
In dimethyl sulfoxide at 60℃; for 4h;	87%
In dimethyl sulfoxide at 60℃; for 4h;	87%
In N,N-dimethyl-formamide Ambient temperature;	84%
In (2S)-N-methyl-1-phenylpropan-2-amine hydrate; N,N-dimethyl-formamide
In N,N-dimethyl-formamide at 20 - 25℃; Product distribution / selectivity;

110-85-0

piperazine

ethyl 5,6-difluoro-1-methyl-4-oxo-4H-<1,3>thiazeto<3,2-a>quinoline carboxylate

113028-17-4

ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate

Conditions

Conditions	Yield
In N,N-dimethyl-formamide at 10 - 55℃; for 9.16667h;	74%

113028-75-4

3,4-difluorophenyl isothiocyanate

113028-17-4

ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate

Conditions

Conditions	Yield
Multi-step reaction with 4 steps 1: 1.) KOH / 1.) dioxane, RT, 30 min., 2.) 4 deg C, 15 h 2: 2.22 g / K2CO3 / dimethylformamide / 1 h / 70 °C 3: 0.350 g / PPE / 1.5 h / 80 °C 4: 84 percent / dimethylformamide / Ambient temperature View Scheme
Multi-step reaction with 6 steps 1: 1.) KOH / 1.) dioxane, RT, 30 min., 2.) 4 deg C, 15 h 2: dimethylformamide / 1.) 0 deg C, 1.5 h, 2.) RT, 2 h 3: 58 percent / diphenyl ether / 5 h / 240 °C 4: 99 percent / 35percent HCl / ethanol / 2 h / Ambient temperature 5: 47 percent / K2CO3, KI / dimethylformamide / 0.5 h / 105 - 110 °C 6: 84 percent / dimethylformamide / Ambient temperature View Scheme

84339-06-0

ethyl 7,6-difluoro-4-hydroxy-2-mercaptoquinoline-3-carboxylate

113028-17-4

ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate

Conditions

Conditions	Yield
Multi-step reaction with 2 steps 1: 47 percent / K2CO3, KI / dimethylformamide / 0.5 h / 105 - 110 °C 2: 84 percent / dimethylformamide / Ambient temperature View Scheme

144514-15-8

3,4-difluorophenyl dithiocarbamic acid triethylammonium

113028-17-4

ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate

Conditions

Conditions	Yield
Multi-step reaction with 5 steps 1: ethyl chloroformate, triethylamine / CHCl3 / 3.5 h / Ambient temperature 2: 1.) KOH / 1.) dioxane, RT, 30 min., 2.) 4 deg C, 15 h 3: 2.22 g / K2CO3 / dimethylformamide / 1 h / 70 °C 4: 0.350 g / PPE / 1.5 h / 80 °C 5: 84 percent / dimethylformamide / Ambient temperature View Scheme
Multi-step reaction with 7 steps 1: ethyl chloroformate, triethylamine / CHCl3 / 3.5 h / Ambient temperature 2: 1.) KOH / 1.) dioxane, RT, 30 min., 2.) 4 deg C, 15 h 3: dimethylformamide / 1.) 0 deg C, 1.5 h, 2.) RT, 2 h 4: 58 percent / diphenyl ether / 5 h / 240 °C 5: 99 percent / 35percent HCl / ethanol / 2 h / Ambient temperature 6: 47 percent / K2CO3, KI / dimethylformamide / 0.5 h / 105 - 110 °C 7: 84 percent / dimethylformamide / Ambient temperature View Scheme

113028-77-6

ethyl 6,7-difluoro-4-hydroxy-2-<(methoxymethyl)thio>-quinoline-3-carboxylate

113028-17-4

ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate

Conditions

Conditions	Yield
Multi-step reaction with 3 steps 1: 99 percent / 35percent HCl / ethanol / 2 h / Ambient temperature 2: 47 percent / K2CO3, KI / dimethylformamide / 0.5 h / 105 - 110 °C 3: 84 percent / dimethylformamide / Ambient temperature View Scheme

144514-35-2

3-(3,4-difluorophenyl)-4-methyl<1,3>thiazetidin-2-ylidenemalonate

113028-17-4

ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate

Conditions

Conditions	Yield
Multi-step reaction with 2 steps 1: 0.350 g / PPE / 1.5 h / 80 °C 2: 84 percent / dimethylformamide / Ambient temperature View Scheme

113028-76-5

diethyl<<(3,4-difluorophenyl)amino><(methoxymethyl)-thio>methylene>malonate

113028-17-4

ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate

Conditions

Conditions	Yield
Multi-step reaction with 4 steps 1: 58 percent / diphenyl ether / 5 h / 240 °C 2: 99 percent / 35percent HCl / ethanol / 2 h / Ambient temperature 3: 47 percent / K2CO3, KI / dimethylformamide / 0.5 h / 105 - 110 °C 4: 84 percent / dimethylformamide / Ambient temperature View Scheme

[[(3,4-difluorophenyl)amino]-mercaptomethylene]-malonic acid diethyl ester potassium salt

113028-17-4

ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate

Conditions

Conditions	Yield
Multi-step reaction with 3 steps 1: 2.22 g / K2CO3 / dimethylformamide / 1 h / 70 °C 2: 0.350 g / PPE / 1.5 h / 80 °C 3: 84 percent / dimethylformamide / Ambient temperature View Scheme
Multi-step reaction with 5 steps 1: dimethylformamide / 1.) 0 deg C, 1.5 h, 2.) RT, 2 h 2: 58 percent / diphenyl ether / 5 h / 240 °C 3: 99 percent / 35percent HCl / ethanol / 2 h / Ambient temperature 4: 47 percent / K2CO3, KI / dimethylformamide / 0.5 h / 105 - 110 °C 5: 84 percent / dimethylformamide / Ambient temperature View Scheme

3863-11-4

3,4-difluoroaniline

113028-17-4

ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate

Conditions

Conditions	Yield
Multi-step reaction with 6 steps 1: 0 °C 2: ethyl chloroformate, triethylamine / CHCl3 / 3.5 h / Ambient temperature 3: 1.) KOH / 1.) dioxane, RT, 30 min., 2.) 4 deg C, 15 h 4: 2.22 g / K2CO3 / dimethylformamide / 1 h / 70 °C 5: 0.350 g / PPE / 1.5 h / 80 °C 6: 84 percent / dimethylformamide / Ambient temperature View Scheme
Multi-step reaction with 8 steps 1: 0 °C 2: ethyl chloroformate, triethylamine / CHCl3 / 3.5 h / Ambient temperature 3: 1.) KOH / 1.) dioxane, RT, 30 min., 2.) 4 deg C, 15 h 4: dimethylformamide / 1.) 0 deg C, 1.5 h, 2.) RT, 2 h 5: 58 percent / diphenyl ether / 5 h / 240 °C 6: 99 percent / 35percent HCl / ethanol / 2 h / Ambient temperature 7: 47 percent / K2CO3, KI / dimethylformamide / 0.5 h / 105 - 110 °C 8: 84 percent / dimethylformamide / Ambient temperature View Scheme

113028-17-4

ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate

112984-60-8

ulifloxacin

Conditions

Conditions	Yield
Stage #1: ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate With water; potassium hydroxide at 80 - 85℃; for 1h; Stage #2: With acetic acid In water at 20℃; for 1h; pH=6.5 - 7;	97%
With water; potassium hydroxide at 60 - 70℃; Large scale;	97.3%
With potassium hydroxide at 20℃; for 5h;	90%
With potassium hydroxide In water; tert-butyl alcohol at 50 - 60℃; for 1h;	88%
Stage #1: ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate With water; potassium hydroxide; tert-butyl alcohol at 20 - 60℃; Stage #2: With water; acetic acid In tert-butyl alcohol

113028-17-4

ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate

598-31-2

1-bromoacetone

ethyl 7-(4-acetonyl-1-piperazinyl)-6-fluoro-1-methyl-4-oxo-4H-<1,3>thiazeto<3,2-a>quinoline-3-carboxylate

Conditions

Conditions	Yield
With triethylamine In N,N-dimethyl-formamide for 4h;	67%
With potassium carbonate In N,N-dimethyl-formamide

80715-22-6

4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one

113028-17-4

ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate

ethyl 6-fluoro-1-methyl-7-<4-<(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl>-1-piperazyl>-4-oxo-4H-<1,3>thiazeto<3,2-a>-quinoline-3-carboxylate

Conditions

Conditions	Yield
With potassium hydrogencarbonate In N,N-dimethyl-formamide for 1h; Ambient temperature;	66%
With potassium hydrogencarbonate In N,N-dimethyl-formamide

113028-17-4

ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate

(pivaloyloxy)methyl 6-fluoro-1-methyl-7-(piperazinyl)-4-oxo-4H-<1,3>thiazeto<3,2-a>quinoline-3-carboxylate

Conditions

Conditions	Yield
Multi-step reaction with 2 steps 1: 88 percent / KOH / 2-methyl-propan-2-ol; H2O / 1 h / 50 - 60 °C 2: 18 percent / K2CO3 / dimethylformamide / 3 h / 60 - 80 °C View Scheme

113028-17-4

ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate

123447-62-1

prulifloxacin

Conditions

Conditions	Yield
Multi-step reaction with 2 steps 1: 88 percent / KOH / 2-methyl-propan-2-ol; H2O / 1 h / 50 - 60 °C 2: 62 percent / KHCO3 / dimethylformamide / 5 h / Ambient temperature View Scheme
Multi-step reaction with 2 steps 1.1: potassium hydroxide; water / 1 h / 80 - 85 °C 1.2: 1 h / 20 °C / pH 6.5 - 7 2.1: N-ethyl-N,N-diisopropylamine / acetonitrile / 0.17 h / 20 °C 2.2: 21 h / 10 - 30 °C View Scheme

80715-22-6

4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one

113028-17-4

ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate

6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl-1-piperazinyl]-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid hydrochloride

Conditions

Conditions	Yield
Stage #1: 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one; ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate With triethylamine In N,N-dimethyl-formamide at 0 - 5℃; Stage #2: With hydrogenchloride In methanol; dichloromethane at 0 - 5℃; Product distribution / selectivity;

113028-17-4Upstream product

• 3863-11-4 3,4-difluoroaniline 
• 110-85-0 piperazine 
• 113028-77-6 ethyl 6,7-difluoro-4-hydroxy-2-<(methoxymethyl)thio>-quinoline-3-carboxylate 
• 84339-06-0 ethyl 7,6-difluoro-4-hydroxy-2-mercaptoquinoline-3-carboxylate 
• 113028-75-4 3,4-difluorophenyl isothiocyanate 
• 113046-72-3 ethyl 6,7-difluoro-1-methyl-4-oxo-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate 
• 113028-76-5 diethyl<<(3,4-difluorophenyl)amino><(methoxymethyl)-thio>methylene>malonate 
• 144514-35-2 3-(3,4-difluorophenyl)-4-methyl<1,3>thiazetidin-2-ylidenemalonate 
• 144514-15-8 3,4-difluorophenyl dithiocarbamic acid triethylammonium 

113028-17-4Downstream Products

• 123447-62-1 prulifloxacin 
• 112984-60-8 ulifloxacin 

113028-17-4Relevant articles and documents

Ulifloxacin hydrochloride crystal and its preparation method and use

-

Paragraph 0061; 0062, (2018/03/01)

The invention provides an ulifloxacin hydrochloride crystal. The X-ray powder diffraction pattern of the ulifloxacin hydrochloride crystal under Cu-K alpha radiation has peaks at 2 theta angles of 8.362+/-0.2 degrees, 9.513+/-0.2 degrees, 12.663+/-0.2 degrees, 21.253+/-0.2 degrees and 24.129+/-0.2 degrees. The invention provides a preparation method of the crystal, a pharmaceutical composition comprising the crystal and a pharmaceutical use of the crystal and the pharmaceutical composition. The ulifloxacin hydrochloride crystal has good reproducibility. The preparation method is simple and reduces the dosage of the organic solvent. Experiments prove that the novel crystal and the mother crystal of ulifloxacin hydrochloride have significant effects in the aspects of solubility, stability, hygroscopicity and in-vivo therapeutic effects. The novel crystal can be processed into a variety of dosage forms and has good clinical application potential.

CRYSTALLINE FORM OF PRULIFLOXACIN AND PROCESSES FOR ITS PREPARATION

-

Page/Page column 21-22, (2012/01/14)

The present invention relates to a crystalline polymorphic form of 6-fluoro-1-methyl-7- {4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]piperazin-1-yl}-4-oxo-4H-[1,3]-thiazeto-[3,2- a]-quinoline-3-carboxylic acid (prulifloxacin). More specifically, the invention relates to a crystalline form of prulifloxacin (herein referred to as Form A), and a method for preparing the crystalline Form A. The present invention further provides a pharmaceutical formulation comprising the novel form of prulifloxacin.

STUDIES ON PYRIDONECARBOXYLIC ACIDS. 1. SYNTHESIS AND ANTIBACTERIAL EVALUATION OF 7-SUBSTITUTED-6-HALO-4-OXO-4H-THIAZETOQUINOLINE-3-CARBOXYLIC ACIDS

Segawa, Jun,Kitano, Masahiko,Kazuno, Kenji,Matsuoka, Masato,Shirahase, Ichiro,et al.

, p. 4727 - 4738 (2007/10/02)

A series of thiazetoquinoline-3-carboxylic acids and their esters were prepared and evaluated for antibacterial activity.The derivatives with a hydrogen or methyl group at C-1, fluorine at C-6, and piperazinyl or 4-methyl-1-piperazinyl group at C-7 showed superior in vitro antibacterial activity, and the derivatives with 4-methyl-1-piperazinyl group at C-7 had potent in vivo activity.Compound 29a (NM394) showed excellent in vitro antibacterial activity and low toxicity but poor absorption from the gastrointestinal tract.Compound 29ee (NM441), an N- derivative of 29a, was found to possess a favorable pharmacokinetic profile and oral activity superior to that of ciprofloxacin in experimental animals.

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