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Basic Information

Molecular Structure:
CAS No.:	82419-36-1
Name:	Ofloxacin
Article Data:	15

Formula:	C₁₈H₂₀FN₃O₄
Molecular Weight:	361.373
Synonyms:	Exocin;Floxin (TN);HOE 280;(+/-)-9-Fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid;Tarivid;DL-8280;Visiren;Prestwick_600;DL 8280;Ocuflox;OFX;Ofloxacin (JP14/USP);ORF 18489;Floxin;OFLX;7H-Pyrido[1,2,3-de]-1,4-benzoxazine-6- carboxylic acid,9-fluoro-2,3-dihydro-3- methyl-10-(4-methyl-1-piperazinyl)-7-oxo-;Ofloxacin (COS);Levoflxacin;
EINECS:	680-263-1
Density:	1.48 g/cm³
Melting Point:	270-275 °C
Boiling Point:	571.5 °C at 760 mmHg
Flash Point:	299.4 °C
Solubility:	Soluble in acetic acid or water. Slightly soluble in methanol
Appearance:	Off-white solid
Hazard Symbols:	Xn, Xi
Risk Codes:	22-42/43-68-36/37/38
Safety:	26-36/37/39-24/25-22-37/39
PSA:	75.01000
LogP:	1.54690

Synthetic route

: 109-01-3
1-methyl-piperazine

: 82419-35-0
9,10-difluoro-2,3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de][1,4]-benzoxazine-6-carboxylic acid

: 82419-36-1
ofloxacin

Conditions

Conditions	Yield
With potassium hydroxide In water at 60℃; for 6h; Time; Solvent;	95.8%
With nano iron oxide on ZrO2 coated sulfonic acid In water for 0.416667h; Reflux;	89%
at 150℃; Microwave irradiation;	83%

: 109-01-3
1-methyl-piperazine

: 82419-34-9
ethyl 9,10-difluoro-3-methyl-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylate

: 82419-36-1
ofloxacin

Conditions

Conditions	Yield
With acetic acid In water; N,N-dimethyl-formamide at 70 - 105℃; for 10h; Temperature; Reagent/catalyst; Solvent;	87.9%

: 139535-20-9
8-Fluoro-3-methyl-9-(4-methyl-piperazin-1-yl)-6-oxo-2,3-dihydro-6H-1-oxa-3a-aza-phenalene-5-carboxylic acid acetoxymethyl ester

: 82419-36-1
ofloxacin

Conditions

Conditions	Yield
With water at 37℃; pH 1.8-10; half-life times;

: 139535-21-0
8-Fluoro-3-methyl-9-(4-methyl-piperazin-1-yl)-6-oxo-2,3-dihydro-6H-1-oxa-3a-aza-phenalene-5-carboxylic acid 1-acetoxy-ethyl ester

: 82419-36-1
ofloxacin

Conditions

Conditions	Yield
With water at 37℃; pH 1.8-10; half-life times;

: 139535-22-1
8-Fluoro-3-methyl-9-(4-methyl-piperazin-1-yl)-6-oxo-2,3-dihydro-6H-1-oxa-3a-aza-phenalene-5-carboxylic acid 1-ethoxycarbonyloxy-ethyl ester

: 82419-36-1
ofloxacin

Conditions

Conditions	Yield
With water at 37℃; pH 1.8-10; half-life times;

: 109-01-3
1-methyl-piperazine

: C13H8BF4NO4

: 82419-36-1
ofloxacin

: 115551-33-2
2-hydroxy 3,4-difluoro aniline

: 82419-36-1
ofloxacin

Conditions

Conditions	Yield
Multi-step reaction with 5 steps 1.1: 80 percent / ethanol / 1 h / Heating 2.1: 95 percent / NaH in oil,; LiClO4 / 18 h / 40 °C 3.1: 80 percent / triphenylphosphine,; DEAD / ethyl acetate / 5 h / 20 °C 4.1: Ac2O,; H2SO4 / 0.75 h / 50 °C 4.2: H2O / 15 h / Heating 5.1: dimethylsulfoxide / 2 h / 100 °C View Scheme

: 85741-74-8
diethyl 2-(((3,4-difluoro-2-hydroxyphenyl)amino)methylene)malonate

: 82419-36-1
ofloxacin

Conditions

Conditions	Yield
Multi-step reaction with 4 steps 1.1: 95 percent / NaH in oil,; LiClO4 / 18 h / 40 °C 2.1: 80 percent / triphenylphosphine,; DEAD / ethyl acetate / 5 h / 20 °C 3.1: Ac2O,; H2SO4 / 0.75 h / 50 °C 3.2: H2O / 15 h / Heating 4.1: dimethylsulfoxide / 2 h / 100 °C View Scheme

: 144298-04-4
(3,4-difluorophenyl)-carbamic acid-tert-butyl ester

: 82419-36-1
ofloxacin

Conditions

Conditions	Yield
Multi-step reaction with 6 steps 1.1: 85 percent 2.1: 80 percent / ethanol / 1 h / Heating 3.1: 95 percent / NaH in oil,; LiClO4 / 18 h / 40 °C 4.1: 80 percent / triphenylphosphine,; DEAD / ethyl acetate / 5 h / 20 °C 5.1: Ac2O,; H2SO4 / 0.75 h / 50 °C 5.2: H2O / 15 h / Heating 6.1: dimethylsulfoxide / 2 h / 100 °C View Scheme

: 86760-99-8
diethyl [(-)-7,8-difluoro-3-methyl-2,3-dihydro-4H-[1,4]benzoxazin-4-yl]methylenemalonate

: 82419-36-1
ofloxacin

Conditions

Conditions	Yield
Multi-step reaction with 2 steps 1.1: Ac2O,; H2SO4 / 0.75 h / 50 °C 1.2: H2O / 15 h / Heating 2.1: dimethylsulfoxide / 2 h / 100 °C View Scheme
Multi-step reaction with 3 steps 1: PPE / 1 h / 140 - 145 °C 2: 94 percent / conc. HCl / acetic acid / 3 h / Heating 3: 62 percent / dimethylsulfoxide / 12 h / 100 - 140 °C View Scheme

Raw Materials

82419-33-8

109-01-3

119-91-5

771-69-7

Downstream Products

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History

OFLOXACIN was developed as a broader-spectrum analog of norfloxacin, the first fluoroquinolone antibiotic, Ofloxacin was first patented in 1982 (European Patent Daiichi) and received U.S. Food and Drug Administration (FDA) approval December 28, 1990. In the United States name branded ofloxacin is rarely used anymore, having been discontinued by the manufacturer (Ortho McNeil Janssen). Johnson and Johnson's annual sales of Floxin in 2003 was approximately $30 million, where as their combined sales of Levaquin/Floxin exceeded $ 1.15 billion in the same year. During the 2008 Johnson & Johnson shareholder’s meetings, the safety of both ofloxacin and levafloxacin were called into question. During the 2009 meeting, yet another shareholder who alleges to have been crippled by these drugs, John Fratti, raised these same issues having seen no significant changes in the warnings (regarding the issues raised during the 2008 meeting). Once again a public request for stronger warnings for both ofloxacin and levofloxacin was made.

Specification

1. Introduction of Ofloxacin
Ofloxacin is one kind of white or almost powder or off-white solid. The Systematic (IUPAC) name of this chemical is (RS)-7-fluoro-2-methyl-6-(4-methylpiperazin-1-yl)-10-oxo-4-oxa-1-azatricyclo[7.3.1.0^5,13]trideca-5(13),6,8,11-tetraene-11-carboxylic acid. Besides, Ofloxacin belongs to Active Pharmaceutical Ingredients;Ofloxacin;Antibiotic Explorer;Intermediates & Fine Chemicals;Pharmaceuticals;1694 Pharmaceuticals&Personal Care Products;Alphabetic;EPA;NeatsAnalytical Standards;O;Peptide Synthesis/Antibiotics;Pharmaceutical intermediate.

The Classification Code of Ofloxacin is Anti-Bacterial Agents; Anti-Infective Agents; Anti-infective agents, urinary; Antibacterial; Drug / Therapeutic Agent; Enzyme Inhibitors; Human Data; Mutation data; Nucleic Acid Synthesis Inhibitors; Renal Agents; Reproductive Effect. Ofloxacin can slightly soluble in water, alcohol, dichloromethane, and methyl alcohol; sparingly soluble in chloroform. Storage of OFLOXACIN: 1. Store at 2-8 ^°C; 2. Keep container tightly closed.

2. Properties of Ofloxacin
Physical properties about Ofloxacin are:
(1)XLogP3: -0.4; (2)H-Bond Donor: 1; (3)H-Bond Acceptor: 8; (4)Molecular Formula: C₁₈H₂₀FN₃O₄; (5)Formula Weight: 361.37; (6)mp: 270-275°C; (7)storage temp.: 2-8°C; (8)Physical State of Ofloxacin: off-white solid.

3. Structure Descriptors of Ofloxacin
(1)InChI: InChI=1S/C18H20FN3O4/c1-10-9-26-17-14-11(16(23)12(18(24)25)8-22(10)14)7-13(19)15(17)21-5-3-20(2)4-6-21/h7-8,10H,3-6,9H2,1-2H3,(H,24,25)
(2)InChIKey: GSDSWSVVBLHKDQ-UHFFFAOYSA-N
(3)Canonical SMILES: CC1COC2=C3N1C=C(C(=O)C3=CC(=C2N4CCN(CC4)C)F)C(=O)O
(4)Smiles: CC1COc2c3n1cc(c(=O)c3cc(c2N4CCN(CC4)C)F)C(=O)O

4. Toxicity of Ofloxacin

Organism	Test Type	Route	Reported Dose (Normalized Dose)	Effect	Source
dog	LD50	intravenous	> 70mg/kg (70mg/kg)		Drugs in Japan Vol. -, Pg. 291, 1995.
dog	LD50	oral	> 200mg/kg (200mg/kg)	GASTROINTESTINAL: CHANGES IN STRUCTURE OR FUNCTION OF SALIVARY GLANDS GASTROINTESTINAL: "HYPERMOTILITY, DIARRHEA"	Chemotherapy Vol. 32(Suppl,
man	TDLo	oral	17mg/kg/3D-I (17mg/kg)	SKIN AND APPENDAGES (SKIN): "DERMATITIS, ALLERGIC: AFTER SYSTEMIC EXPOSURE" BEHAVIORAL: EXCITEMENT BLOOD: CHANGES IN CELL COUNT (UNSPECIFIED)	Internal Medicine. Vol. 34, Pg. 872, 1995.
man	TDLo	oral	51428ug/kg (51.428mg/kg)	GASTROINTESTINAL: "HYPERMOTILITY, DIARRHEA"	American Journal of Medicine. Vol. 87, Pg. 479, 1989.
monkey	LD50	oral	500mg/kg (500mg/kg)		Chemotherapy Vol. 32(Suppl,
mouse	LD50	intramuscular	> 600mg/kg (600mg/kg)	BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD	Zhongguo Kangshengsu Zazhi. Chinese Journal of Antibiotics. Vol. 18, Pg. 218, 1993.
mouse	LD50	intraperitoneal	805mg/kg (805mg/kg)		Ensho. Japanese Journal of Inflammation. Vol. 11, Pg. 343, 1991.
mouse	LD50	intravenous	208mg/kg (208mg/kg)	LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD BEHAVIORAL: COMA	Chemotherapy Vol. 32(Suppl,
mouse	LD50	oral	3266mg/kg (3266mg/kg)	BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD	Zhongguo Kangshengsu Zazhi. Chinese Journal of Antibiotics. Vol. 18, Pg. 218, 1993.
mouse	LDLo	subcutaneous	7690mg/kg (7690mg/kg)		Chemotherapy Vol. 32(Suppl,
rat	LD50	intravenous	273mg/kg (273mg/kg)	BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD BEHAVIORAL: COMA LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION	Chemotherapy Vol. 32(Suppl,
rat	LD50	oral	3590mg/kg (3590mg/kg)	BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD BEHAVIORAL: ATAXIA LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION	Chemotherapy Vol. 32(Suppl,
rat	LD50	subcutaneous	7070mg/kg (7070mg/kg)	BEHAVIORAL: ATAXIA BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION	Chemotherapy Vol. 32(Suppl,
women	TDLo	oral	24mg/kg/3D-I (24mg/kg)	BEHAVIORAL: TOXIC PSYCHOSIS BEHAVIORAL: "HALLUCINATIONS, DISTORTED PERCEPTIONS" BEHAVIORAL: IRRITABILITY	Journal of Clinical Psychiatry. Vol. 53, Pg. 137, 1992

1.	dnd-hmn:lym 80 mg/L	MUREAV Mutation Research. 211 (1989),171.
2.	orl-wmn TDLo:24 mg/kg/3D-I:BAH	JCLPDE Journal of Clinical Psychiatry. 53 (1992),137.
3.	orl-man TDLo:51,428 µg/kg:GIT	AJMEAZ American Journal of Medicine. 87 (1989),479.
4.	orl-rat LD50:3590 mg/kg	NKRZAZ Chemotherapy (Tokyo). 32 (Suppl 1)(1984),1084.
5.	scu-rat LD50:7070 mg/kg	NKRZAZ Chemotherapy (Tokyo). 32 (Suppl 1)(1984),1084.
6.	ivn-rat LD50:273 mg/kg	NKRZAZ Chemotherapy (Tokyo). 32 (Suppl 1)(1984),1084.
7.	orl-mus LD50:5290 mg/kg	NKRZAZ Chemotherapy (Tokyo). 32 (Suppl 1)(1984),1084.
8.	scu-mus LDLo:7690 mg/kg	NKRZAZ Chemotherapy (Tokyo). 32 (Suppl 1)(1984),1084.
9.	ivn-mus LD50:208 mg/kg	NKRZAZ Chemotherapy (Tokyo). 32 (Suppl 1)(1984),1084.
10.	ivn-dog LDLo:100 mg/kg	NKRZAZ Chemotherapy (Tokyo). 32 (Suppl 1)(1984),1084.
11.	orl-mky LD50:500&

5. Safety information of Ofloxacin
Hazard Codes :

Xn,

Xi
Risk Statements : 22-42/43-68-36/37/38
Safety Statements : 26-36/37/39-24/25-22-37/39
1.Do not breathe dust.
2.Avoid contact with skin. S24/25 Avoid contact with skin and eyes.
3.Avoid contact with eyes.
WGK Germany : 3
RTECS : UU8815550
Poison by intravenous route. Moderately toxic by ingestion. An experimental teratogen. Other experimental reproductive effects. Human systemic effects: body temperature increase, diarrhea, hallucinations, hypermotility, irritability, psychosis. Mutation data reported. When heated to decomposition it emits toxic fumes of F⁻ and NO_x.

6. Physical Properties of Ofloxacin

Physical Property	Value	Units	Temp (deg C)	Source
Melting Point	254 dec	deg C		EXP
log P (octanol-water)	-0.39	(none)		EXP
Water Solubility	2.83E+04	mg/L	25	EST
Vapor Pressure	1.55E-13	mm Hg	25	EST
Henry's Law Constant	4.98E-20	atm-m3/mole	25	EST
Atmospheric OH Rate Constant	1.97E-10	cm3/molecule-sec	25	EST

7. Uses of Ofloxacin
OFLOXACIN can be used as fluorinated quinolone antibacterial. A synthetic fluoroquinolone (FLUOROQUINOLONES) antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.

8. Production of Ofloxacin
(1) 2,3,4-trifluoronitrobenzene as the starting material by selective alkaline hydrolysis, etherification, restore, and C₂H₅OCH=C(COOEt)₂ or (CH₃)₂NCH=C (COOEt)₂ condensation ringaggregate, after hydrolysis with acetic acid boron role, and then the introduction of N-methyl-piperazine-derived products.

Production of Ofloxacin

(2) Phthalimide derivative as a raw material generated by fluorination tetrafluorophthalic phthalimide, hydrolysis, decarboxylation of 2,3,4,5-tetrafluoro-benzoic acid, and then chlorinated, acylatingdecarboxylated 2,3,4,5-tetrafluorobenzoyl ethyl acetate, and then the first and of triethyl orthoformate, and after 2-aminopropanol reaction, and then cyclization generated pyridine [1,2,3-de] [1,4] benzo Hey triazine derivatives, and finally reaction of ofloxacin and piperazine.

Production of Ofloxacin