16773-42-5

Basic information

• Product Name: Ornidazole
• Synonyms: alpha-(chlormethyl)-2-methyl-5-nitro-imidazol-1-aethanol;alpha-(chloromethyl)-2-methyl-5-nitro-1h-imidazole-1-ethano;alpha-(chloromethyl)-2-methyl-5-nitro-imidazole-1-ethano;ro7-0207;tiberal;ORNIDAZOLE;TIMTEC-BB SBB006918;LABOTEST-BB LT00772185
• CAS NO: 16773-42-5
• Molecular Formula: C₇H₁₀ClN₃O₃
• Molecular Weight: 219.63
• EINECS: 240-826-0
• Product Categories: Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Intermediates & Fine ChemicalsHeterocycles;API;alcohol| alkyl chloride| nitro-compound;OGEN;disinfectant
• Mol File: 16773-42-5.mol

Chemical Properties

• Melting Point: 85-90°C
• Boiling Point: 443.2 ºC at 760 mmHg
• Flash Point: 221.9 ºC
• Appearance: Crystalline solid
• Density: 1.6545 (rough estimate)
• Vapor Pressure: 1.23E-08mmHg at 25°C
• Refractive Index: 1.6000 (estimate)
• Storage Temp.: -20°C Freezer
• Solubility: Soluble in ethanol at 50mg/ml
• PKA: 2.4 ± 0.1(at 25℃)
• Merck: 14,6872
• CAS DataBase Reference: Ornidazole(CAS DataBase Reference)
• NIST Chemistry Reference: Ornidazole(16773-42-5)
• EPA Substance Registry System: Ornidazole(16773-42-5)

Safety Data

• Hazard Codes: Xn
• Statements: 22
• Safety Statements: 36
• WGK Germany: 3
• RTECS: NI5460000
• HazardClass: IRRITANT
• Hazardous Substances Data: 16773-42-5(Hazardous Substances Data)

Usage

Uses

Used in Anti-infective Applications:
Ornidazole is used as an anti-infective agent for treating a range of infections, including mixed amoebiasis, mixed amoebic dysentery, mixed giardiasis, trichomoniasis, bacterial vaginosis, sexually transmitted diseases, infections of gynecology, lower respiratory tract infections, ENT, surgical, and dental infections. It is effective against clinical isolates of B. fragilis, various anaerobic bacteria, and Giardia isolates.
Used in Crohn's Disease Treatment:
Ornidazole has been investigated for use in Crohn's disease after bowel resection, providing a potential therapeutic option for patients suffering from this condition.
Used in Estrogen Regulation:
Ornidazole has been shown to induce infertility in male rats within 7 days and inhibit spermatozoa binding to rat oocyte zona pellucida, suggesting a potential role in estrogen regulation and fertility control.
Used in Pharmaceutical Industry:
Ornidazole is used in the pharmaceutical industry for the treatment of susceptible protozoal infections and anaerobic bacterial infections, offering a valuable treatment option for patients suffering from these conditions.

Indications

Ornidazole is given to patients who have vaginal infections such as bacterial vaginitis, post-surgical infections, anaerobic bacterial infections, skin infections, trichomonas vaginitis, intestinal infections, stomach infections, parasitic infections and bacterial infections. It is highly recommended that this drug is taken under appropriate diagnosis and medical indication.

Contraindications

It is not recommended to take this medicine if one is hypersensitive to similar antibiotics, or if one has a history of hypersensitivity. Other than hypersensitivity, this drug is contraindicated in lactating/pregnant women, and in patients with epilepsy, myasthenia gravis and multiple sclerosis.

Dosage Information

For the treatment of amoebiasis, adult patients should take 1g daily in 2 doses for 7-10 days whereas children should be given 10-25mg/kg once a day for 3 days. For treatment of amoebic dysentery, adults should take 1.5mg once a day for 3 days whereas children should be given 40mg/kg once per day for 3 days. The typical Ornidazole dosage for treatment of trichomoniasis in adults is 0.5gm once every 12 hours/1.5gm as a single dose for 5 days. In children, 25mg/kg can be taken as a single dose. For treatment of Giardiasis in adults, 1-1.5gm should be taken once per day for 2 days and in children, 40mg/kg should be taken for two days. The dosage requirements for the treatment of bacterial vaginitis is 1.5gm, which is taken once every day or 500mg taken as a daily single dose for 5-7 days. In the event of a missed dose, supportive and symptomatic treatment should be commenced where the Ornidazole is removed through gastric lavage, induced emesis, application of a carthartic or administration of activated charcoal.

Mechanism of Action

The drug is a nitroimidazole with broad spectrum cidal action against specific types of anaerobic bacteria and protozoa. Ornidazole’s selective toxicity in response to anaerobic microbes entails entry of the drug into the cell through diffusion and reduction of the drug’s nitro group into reactive nitro by redox proteins in anaerobic organisms. This activity influences cytotoxic action by destroying DNA and other fundamental molecules. The final step entails destabilization of the DNA helix and the breakage of certain strands.

Drug Interactions

Some medications have a higher probability of interacting with other prescription drugs hence the doctor should approve any medication adjustments. It is essential for a patient to notify their doctor of any medication, herbal treatments and vitamin supplements that they may be taking before the administration of Ornidazole. A prompt notification may minimize the probability of occurrence of specific side effects. Ornidazole may interact with warfarin and vecuronium.

Warnings

It is recommended that a patient abstains from alcohol intake for at least 3 days after initiation of therapy with this drug. Alcohol use or associated products may influence disulfiram-like responses in some people. Ornidazole use in pregnant/breastfeeding women is not recommended as the potential risks may outweigh the benefits in some cases. However, a patient should always consult their healthcare practitioner before taking this medication. The use of Ornidazole may result in drowsiness hence a patient should avoid activities such as the operation of heavy machinery and driving during the first stages of treatment with this drug. Caution should be taken amongst patients with multiple sclerosis as it is a neurodegenerative disorder associated with the brain. Ornidazole should not be prescribed for patients with convulsion disorders such as epilepsy. For patients with hepatic/renal impairment, the drug should be used cautiously as it may intensify the severity of the pre-existing condition. In this case, it is recommended that the patient is monitored frequently by their doctor for mild to moderate impairment and the respective dose modifications.

Pharmacokinetics

Ornidazole is absorbed well orally, and it is widely distributed through the body. The drug undergoes metabolism in the liver and part of the drug is excreted in bile whereas the rest is eliminated in urine. The duration of action of the drug is 14 hours.

Side Effects

In the administration of medications to treat specific medical conditions, there is a high probability that unintended side effects will develop. Patients on Ornidazole treatment may experience some of the associated side effects in varying intensities. However, if the symptoms persist for an extended period, the patient should contact their doctor. Potential side effects may include hormonal imbalances in the thyroid gland, skin rash, urticaria, abdominal distress, vertigo metallic taste, dry mouth, upset stomach, drowsiness, headache and nausea.

Originator

Tiberal,Roche,W. Germany ,1977

Manufacturing Process

5g of 1-(2,3-epoxypropyl)-2-methyl-5-nitroimidazole was added to 30 ml of concentrated aqueous hydrochloric acid. The solution was heated to the boiling point for 20 minutes, chilled, diluted with 30 ml of water and carefully neutralized with ammonia to a pH of 7 to 8. It was then saturated with ammonium sulfate. The precipitated oil crystallized after several days. Recrystallized from toluene, there was obtained the 1-(3-chloro-2hydroxypropyl)-2-methyl-5-nitroimidazole product melting at 77°C to 78°C.

Therapeutic Function

Antiinfective

Pharmaceutical Applications

A 5-nitroimidazole available for oral administration, intravenous infusion and as a vaginal pessary. Its activity closely parallels that of metronidazole and tinidazole.Peak plasma levels after a single 750 mg or 1.5 g oral dose reach 11 mg/L and 30 mg/L, respectively, within about 2 h. The half-life is 12–14 h. It is well absorbed from the vagina, with peak plasma concentrations of 5 mg/L being reached 12 h after the insertion of a 500 mg vaginal pessary. After a single 1 g intravenous infusion for colorectal surgery, serum levels reached about 24 mg/L after 15 min and about 6 mg/L after 24 h. It has wide tissue distribution, including CSF. Plasma protein binding is 10–15%.It is metabolized in the liver, mainly to hydroxymethyl derivatives. The plasma clearance rate decreases in hepatic failure because of reduced liver metabolism and decreased biliary elimination. About 60% of an oral dose is recovered in the urine and 20% in the feces. The dosing interval should be doubled in patients with severe hepatic impairment, but it is unnecessary to reduce the dose in patients with impaired renal function. It is removed by hemodialysis.Toxicity and side effects are similar to those of metronidazole and tinidazole and it has similar clinical uses. It has been shown to be effective for the prevention of recurrence of Crohn’s disease after ileocolonic resection.

Safety Profile

Poison by intravenous route. Moderately toxic by ingestion and intraperitoneal routes. Experimental reproductive effects. Mutation data reported. Whenheated to decomposition it emits very toxic fumes of Clí and NOx.

InChI:InChI=1/C7H10ClN3O3/c1-5-9-3-7(11(13)14)10(5)4-6(12)2-8/h3,6,12H,2,4H2,1H3

Synthetic route

2-methyl-5-nitro-1H-imidazole (696-23-1) + epichlorohydrin (106-89-8) → ornidazole (16773-42-5)

Conditions	Yield
With 1-[3,5-bis(trifluoromethyl)phenyl]-3-[2-(dimethylamino)cyclohexyl]thiourea In ethyl acetate at 25 - 30℃; for 6h; Solvent; Temperature; Reagent/catalyst;	85.2%
Stage #1: 2-methyl-5-nitro-1H-imidazole With aluminum (III) chloride In ethyl acetate at 0℃; for 0.25h; Stage #2: epichlorohydrin In ethyl acetate	79%
With aluminum (III) chloride In ethyl acetate at 45 - 50℃; for 1.5h;	78%

ornidazole (16773-42-5) → (±)-2-methyl-5-nitro-1-(oxiran-2-ylmethyl)-1H-imidazole (16773-52-7)

Conditions	Yield
With sodium hydroxide In water; acetone at 0℃; for 1h; Inert atmosphere;	97.2%
With sodium hydroxide In dichloromethane; water at 0℃;	91%
With sodium hydroxide In dichloromethane at 0℃; for 3h;	90%
With sodium hydroxide for 0.25h;	82%

ornidazole (16773-42-5) + gatifloxacin (160738-57-8, 112811-59-3) → 1-cyclopropyl-6-fluoro-7-(4-(2-hydroxy-3-(2-methyl-5-nitro-1H-imidazol-1-yl)propyl)-3-methylpiperazin-1-yl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

Conditions	Yield
With potassium hydroxide In ethanol; water for 12h; Reflux;	93%

potassium tetrachloroplatinate(II) (10025-99-7) + ornidazole (16773-42-5) → (NO2CCHNC(CH3)N(CH2CH(OH)CH2Cl))2PtCl2 (84431-20-9)

Conditions	Yield
In water solid ligand added to aq. soln. of K2(PtCl4), stirred at 50 °C for 1 h; ppt. filtered, washed with EtOH/Et2O, Et2O, dried in vac.; elem. anal.;	91%

ornidazole (16773-42-5) + 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-7-(3-methylaminopiperidin-1-yl)-3-quinolinecarboxylic acid → 1-cyclopropyl-6-fluoro-7-(3-((2-hydroxy-3-(2-methyl-5-nitro-1H-imidazol-1-yl)propyl)(methyl)amino)piperidin-1-yl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

Conditions	Yield
With potassium hydroxide In ethanol; water for 12h; Reflux;	91%

moxifloxacin hydrochloride + ornidazole (16773-42-5) → 1-cyclopropyl-6-fluoro-7-((4aS,7aS)-1-(2-hydroxy-3-(2-methyl-5-nitro-1H-imidazol-1-yl)propyl)hexahydro-1H-pyrrolo[3,4-b]pyridin-6(2H)-yl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

Conditions	Yield
With potassium hydroxide In ethanol; water for 12h; Reflux;	87%

ornidazole (16773-42-5) → C14H19Cl2N6O8P

Conditions	Yield
With trichlorophosphate In acetonitrile Reflux;	87%

acetic anhydride (108-24-7) + ornidazole (16773-42-5) → 1-(2-acetoxypropyl-3-chloro)-2-methyl-5-nitroimidazole (57939-59-0)

Conditions	Yield
With pyridine for 1h; Ambient temperature;	84%

ornidazole (16773-42-5) + potassium 4-benzylpiperidinedithiocarbamate → (±)-2-hydroxy-3-(2-methyl-5-nitro-1H-imidazol-1-yl)propyl 4-benzylpiperidine-1-carbodithioate

Conditions	Yield
In acetone for 4h; Alkylation; Heating;	81%

ornidazole (16773-42-5) + 4-phenyl-5-(2-thienyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione → 1-(2-methyl-5-nitro-imidazol-1-yl)-3-(4-phenyl-5-thiophen-2-yl-4H-[1,2,4]triazol-3-ylsulfanyl)-propan-2-ol

Conditions	Yield
With potassium carbonate In acetone for 21h; Alkylation; Heating;	81%

ornidazole (16773-42-5) + 4-(4-fluoro-phenyl)-5-furan-2-yl-2,4-dihydro-[1,2,4]triazole-3-thione → 1-[4-(4-fluoro-phenyl)-5-furan-2-yl-4H-[1,2,4]triazol-3-ylsulfanyl]-3-(2-methyl-5-nitro-imidazol-1-yl)-propan-2-ol

Conditions	Yield
With potassium carbonate In acetone for 21h; Alkylation; Heating;	81%

ornidazole (16773-42-5) + 4-cyclohexyl-5-(2-furyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione → 1-(4-cyclohexyl-5-furan-2-yl-4H-[1,2,4]triazol-3-ylsulfanyl)-3-(2-methyl-5-nitro-imidazol-1-yl)-propan-2-ol

Conditions	Yield
With potassium carbonate In acetone for 21h; Alkylation; Heating;	80%

ornidazole (16773-42-5) + 4-ethyl-2,4-dihydro-5-(2-furyl)-3H-1,2,4-triazole-3-thione → 1-(4-ethyl-5-furan-2-yl-4H-[1,2,4]triazol-3-ylsulfanyl)-3-(2-methyl-5-nitro-imidazol-1-yl)-propan-2-ol

Conditions	Yield
With potassium carbonate In acetone for 21h; Alkylation; Heating;	79%

ornidazole (16773-42-5) + 5-(2-furyl)-4-phenyl-2,4-dihydro-1,2,4-triazole-3-thione → 1-(5-furan-2-yl-4-phenyl-4H-[1,2,4]triazol-3-ylsulfanyl)-3-(2-methyl-5-nitro-imidazol-1-yl)-propan-2-ol

Conditions	Yield
With potassium carbonate In acetone for 21h; Alkylation; Heating;	78%

copper(II) acetate monohydrate (6046-93-1) + ornidazole (16773-42-5) → [Cu2(acetate)4(1-chloro-3-(2-methyl-5-nitro-1H-imidazol-1-yl)propan-2-ol)2]

Conditions	Yield
In methanol at 60℃; for 6h; Reflux;	78%

2-nitro-aniline (88-74-4) + ornidazole (16773-42-5) → C13H15N5O5

Conditions	Yield
In propan-1-ol for 64h; Reflux;	77%

ornidazole (16773-42-5) + phenol (108-95-2) → 1-(3'-phenoxy-2'-hydroxypropyl)-2-methyl-5-nitroimidazole (19180-02-0)

Conditions	Yield
With potassium carbonate In propan-1-ol for 12h; Heating;	76.4%

ornidazole (16773-42-5) + 5-(2-furyl)-4-(4-chlorophenyl)-2,4-dihydro-1,2,4-triazole-3-thione → 1-[4-(4-chloro-phenyl)-5-furan-2-yl-4H-[1,2,4]triazol-3-ylsulfanyl]-3-(2-methyl-5-nitro-imidazol-1-yl)-propan-2-ol

Conditions	Yield
With potassium carbonate In acetone for 21h; Alkylation; Heating;	76%

ornidazole (16773-42-5) + 4-(4-bromophenyl)-5-(furan-2-yl)-2,4-dihydro-3H-1,2,4-triazole-3-thione → 1-[4-(4-bromo-phenyl)-5-furan-2-yl-4H-[1,2,4]triazol-3-ylsulfanyl]-3-(2-methyl-5-nitro-imidazol-1-yl)-propan-2-ol

Conditions	Yield
With potassium carbonate In acetone for 21h; Alkylation; Heating;	75%

4-chloro-aniline (106-47-8) + ornidazole (16773-42-5) → C13H15ClN4O3

Conditions	Yield
In propan-1-ol for 64h; Reflux;	73%

ornidazole (16773-42-5) + 4-(4-chlorophenyl)-5-(thiophen-2-yl)-2,4-dihydro-3 H-1,2,4-triazole-3-thione → 1-[4-(4-chloro-phenyl)-5-thiophen-2-yl-4H-[1,2,4]triazol-3-ylsulfanyl]-3-(2-methyl-5-nitro-imidazol-1-yl)-propan-2-ol

Conditions	Yield
With potassium carbonate In acetone for 21h; Alkylation; Heating;	71%

ornidazole (16773-42-5) → 1-(3-chloro-2-hydroxypropyl)-2-methyl-5-aminoimidazole

Conditions	Yield
With hydrogen In para-xylene at 130℃; under 750.075 Torr; for 24h; chemoselective reaction;	71%
With hydrogenchloride; zinc In ethanol
With sulfuric acid In methanol; water at 25℃; Electrochemical reaction;

isopropylamine (75-31-0) + ornidazole (16773-42-5) → 1-(3'-isopropylamino-2'-hydroxypropyl)-2-methyl-5-nitroimidazole

Conditions	Yield
In propan-1-ol for 4h; Heating;	70.17%

aniline (62-53-3) + ornidazole (16773-42-5) → 1-(3'-anilino-2'-hydroxypropyl)-2-methyl-5-nitroimidazole

Conditions	Yield
In propan-1-ol for 4h; Heating;	70.17%

ornidazole (16773-42-5) + 4-allyl-5-furan-2-yl-2,4-dihydro-[1,2,4]triazole-3-thione → 1-(4-allyl-5-furan-2-yl-4H-[1,2,4]triazol-3-ylsulfanyl)-3-(2-methyl-5-nitro-imidazol-1-yl)-propan-2-ol

Conditions	Yield
With potassium carbonate In acetone for 21h; Alkylation; Heating;	70%

ornidazole (16773-42-5) + 4-butyl-5-furan-2-yl-2,4-dihydro-[1,2,4]triazole-3-thione → 1-(4-butyl-5-furan-2-yl-4H-[1,2,4]triazol-3-ylsulfanyl)-3-(2-methyl-5-nitro-imidazol-1-yl)-propan-2-ol

Conditions	Yield
With potassium carbonate In acetone for 21h; Alkylation; Heating;	70%

4-nitro-aniline (100-01-6) + ornidazole (16773-42-5) → C13H15N5O5

Conditions	Yield
In propan-1-ol for 64h; Reflux;	68%

prulifloxacin (123447-62-1) + ornidazole (16773-42-5) → 6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-[1,3]dioxol-4-ylmethyl)piperazin-1-yl]-4-oxo-4H-2-thia-8b-aza-cycobuta[a]naphthalene-3-carboxylic acid 1-chloromethyl-2-(2-methyl-5-nitro-imidazol-1-yl)ethyl ester

Conditions	Yield
With dmap; benzotriazol-1-ol; dicyclohexyl-carbodiimide In N,N-dimethyl-formamide at 20℃; for 16h;	65%

ornidazole (16773-42-5) + m,p-dichloroaniline (95-76-1) → C13H14Cl2N4O3

Conditions	Yield
In propan-1-ol for 64h; Reflux;	65%

ornidazole (16773-42-5) + 4-bromo-aniline (106-40-1) → C13H15BrN4O3

Conditions	Yield
In propan-1-ol for 64h; Reflux;	64%

Upstream product

• 696-23-1 2-methyl-5-nitro-1H-imidazole 
• 106-89-8 epichlorohydrin 
• 67843-74-7 (S)-epichlorohydrin 
• 16773-42-5 ornidazole 

Downstream Products

• 16773-52-7 (±)-2-methyl-5-nitro-1-(oxiran-2-ylmethyl)-1H-imidazole 
• 166734-83-4 (R)-1-chloro-3-(2-methyl-5-nitro-1H-imidazol-1-yl)propan-2-ol 
• 19180-00-8 1-(2-methyl-5-nitro-imidazol-1-yl)-3-o-tolyloxy-propan-2-ol 
• 19180-01-9 1-(2-chloro-phenoxy)-3-(2-methyl-5-nitro-imidazol-1-yl)-propan-2-ol 
• 19180-02-0 1-(3'-phenoxy-2'-hydroxypropyl)-2-methyl-5-nitroimidazole 
• 16773-42-5 (S)-(-)-1-(3-chloro-2-hydroxypropyl)-2-methyl-5-nitroimidazole 

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Effects of the Ornidazole (cas 16773-42-5) enantiomers on the central nervous system: Involvement of the GABAA receptor07/20/2019

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Relevant articles and documents

Nitroimidazole derivative, preparation method and application thereof

The invention provides a nitroimidazole derivative as shown in a general formula I or a pharmaceutically acceptable salt, a solvent compound, a hydrate, a polymorphic substance, a deuterated substance and an isomer thereof. The invention also provides a pharmaceutical composition containing the compound and application of the pharmaceutical composition. The nitroimidazole derivative provided by the invention has excellent pharmacokinetic properties, and also has excellent antibacterial activity.

Preparation method of optically active ornidazole

The invention relates to the technical field of organic chemical synthesis, in particular to a preparation method of optically active ornidazole. According to the preparation method, 2-methyl-5-nitroimidazole and optically active epoxy chloropropane are used as raw materials, an acid solvent is used as a reaction solvent, Lewis acid is used as a catalyst, a reaction is carried out under the condition close to normal temperature, and then extraction is carried out to obtain the product. Compared with the traditional optically active ornidazole synthesis process, the preparation method has theadvantages that the use of aluminum trichloride is avoided, the pollution of aluminum salt to the environment is reduced, low-temperature control in the reaction process is not needed, the reaction conditions are mild and easy to control, the temperature control cost can be reduced, the types of solvents are fewer, the operation is simple, and the cost is lower; and the method is suitable for industrial production of optically active ornidazole.

Novel chiral stationary phases based on 3,5-dimethyl phenylcarbamoylated β-cyclodextrin combining cinchona alkaloid moiety

Novel chiral selectors based on 3,5-dimethyl phenylcarbamoylated β-cyclodextrin connecting quinine (QN) or quinidine (QD) moiety were synthesized and immobilized on silica gel. Their chromatographic performances were investigated by comparing to the 3,5-dimethyl phenylcarbamoylated β-cyclodextrin (β-CD) chiral stationary phase (CSP) and 9-O-(tert-butylcarbamoyl)-QN-based CSP (QN-AX). Fmoc-protected amino acids, chiral drug cloprostenol (which has been successfully employed in veterinary medicine), and neutral chiral analytes were evaluated on CSPs, and the results showed that the novel CSPs characterized as both enantioseparation capabilities of CD-based CSP and QN/QD-based CSPs have broader application range than β-CD-based CSP or QN/QD-based CSPs. It was found that QN/QD moieties play a dominant role in the overall enantioseparation process of Fmoc-amino acids accompanied by the synergistic effect of β-CD moiety, which lead to the different enantioseparation of β-CD-QN-based CSP and β-CD-QD-based CSP. Furthermore, new CSPs retain extraordinary enantioseparation of cyclodextrin-based CSP for some neutral analytes on normal phase and even exhibit better enantioseparation than the corresponding β-CD-based CSP for certain samples.

Process for preparing 5-nitroimidazole medicine through catalysis of small organic molecules

The invention provides a process for preparing a 5-nitroimidazole medicine through catalysis of small organic molecules. The preparation method comprises the following steps: 1) uniformly stirring andmixing 2-methyl-5-nitroimidazole, a solvent and a catalyst which is selected from 1-(3, 5-ditrifluoromethyl phenyl)-3-(2-dimethylamino-cyclohexyl)-thiourea, and 2) adding epoxy chloropropane or epoxypropane into a reaction system in the step 1), and reacting to obtain the 5-nitroimidazole medicine. According to the present invention, the 5-nitroimidazole medicine prepared by using the synthesisprocess has characteristics of low catalyst consumption, high catalytic activity, high reaction selectivity, high yield, easy catalyst recycling, and environmental protection.

Synthesis method of 5-nitroimidazole drugs

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Nitroimidazole derivative, preparation method and applications thereof

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High-safety L-ornidazole injection and preparation method thereof

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Novel nitroimidazole drug as well as preparation method and application of novel nitroimidazole drug

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The invention provides an s-ornidazole injection with high safety. The s-ornidazole injection is prepared from components of s-ornidazole and an isoosmotic adjusting agent; the s-ornidazole injection is characterized in that the s-ornidazole injection contains acetamide, wherein the content of the acetamide is not higher than 10 mg/l. The s-ornidazole injection provided by the invention is high in safety and low in toxicity, and is capable of well exerting the clinical effects of the s-ornidazole.

After-treatment method for levornidazole reaction liquid

The invention discloses an after-treatment method for levornidazole reaction liquid and belongs to the technical field of medicine synthesis. The method includes the steps of 1) adding 2-methyl-5-nitroimidazole to ethyl acetate; 2) under catalysis of aluminum chloride, adding S-epoxychloropropane to perform a reaction to obtain a reaction liquid; 3) quenching the reaction liquid in ice water, separating the reaction liquid to obtain an ethyl acetate phase, and drying the ethyl acetate phase and performing pressure-reduced concentration to obtain an oily substance; 4) adding an organic solvent to the oily substance and pulping the mixture, adding a low-polar solvent to further separate a solid out; and 5) filtering and drying the solid to obtain levornidazole. The after-treatment method is free of addition of acid and alkali for regulating pH value, so that generation of a thermal degradation impurity due to acid-base neutralization heat release can be avoided. The method is simple in operation, is high in yield and is suitable for industrial production.