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ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate

Flumazenil

CAS: 78755-81-4

Molecular Formula: C15H14FN3O3

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ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate - Names and Identifiers

Name Flumazenil
Synonyms FMZ
RO15-1788
FLUMAZENIL
RO 15-1788
Ro 15-1788
Flumazenil
FluMazenil USP
ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4h-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
8-FLUORO-5,6-DIHYDRO-5-METHYL-6-OXO-4H-IMIDAZO[1,5-A][1,4]BENZODIAZEPINE-3-CARBOXYLIC ACID ETHYL EST
8-FLUORO-5,6-DIHYDRO-5-METHYL-6-OXO-4H-IMIDAZO[1,5-A][1,4]BENZO-DIAZEPINE-3-CARBOXYLIC ACID ETHYL ESTER
4H-IMIDAZO[1,5-A][1,4]BENZODIAZEPINE-3-CARBOXYLIC ACID, 8-FLUORO-5,6-DIHYDRO-5-METHYL-6-OXO-, ETHYL ESTER
8-Fluoro-5,6-dihydro-5-methyl-6-oxo-4H- Imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid ethyl ester
CAS 78755-81-4
EINECS 616-650-9
InChI InChI=1/C15H14FN3O3/c1-3-22-15(21)13-12-7-18(2)14(20)10-6-9(16)4-5-11(10)19(12)8-17-13/h4-6,8H,3,7H2,1-2H3

ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate - Physico-chemical Properties

Molecular FormulaC15H14FN3O3
Molar Mass303.29
Density1.39±0.1 g/cm3(Predicted)
Melting Point201-203°C
Boling Point528.0±50.0 °C(Predicted)
Flash Point273.1°C
Water Solubility128 mg/L
Solubility Soluble in DMSO to 25mM
Vapor Presure3.1E-11mmHg at 25°C
Appearancesolid | white
Colorwhite
Merck14,4135
pKa0.86±0.20(Predicted)
Storage ConditionSealed in dry,2-8°C
StabilityStable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Refractive Index1.633
MDLMFCD00242764
Physical and Chemical PropertiesCrystallization in alcohol, melting point 20l ~ 203 deg C. Acute toxicity LD50 mice, rats (mg/kg):4000,1360 intraperitoneal injection; 4300,6000 oral.

ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate - Risk and Safety

Hazard SymbolsXi - Irritant
Irritant
Risk Codes36/37/38 - Irritating to eyes, respiratory system and skin.
Safety DescriptionS26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
S27 - Take off immediately all contaminated clothing.
S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection.
WGK Germany2
RTECSNI2922170
HS Code2933997500
ToxicityLD50 in mice, rats (mg/kg): 4000, 1360 i.p.; 4300, 6000 orally (Hunkeler)

ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate - Standard

Authoritative Data Verified Data

This product is 8-fluoro-5, 6-dihydro-5-methyl-6-oxo-4h-imidazo-[1,5-a][1,4] benzodiazepane-3-carboxylic acid ethyl ester. Calculated as dry product, containing no less than 99.0% of C15H14FN3O3.

Last Update：2024-01-02 23:10:35

ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate - Trait

Authoritative Data Verified Data
  • This product is white or off-white crystalline powder; Odorless.
  • This product is soluble in chloroform or glacial acetic acid, slightly soluble in methanol, almost insoluble in water.

melting point

The melting point of this product (General rule 0612 first method) is 198~202°C, and it is decomposed at the same time during melting.

Last Update：2022-01-01 13:40:22

ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate - Differential diagnosis

Authoritative Data Verified Data
  1. take about 10mg of this product, Dropwise add glacial acetic acid to make it just soluble, add dilute bismuth potassium iodide solution to generate orange red precipitate.
  2. This product is dissolved in methanol and diluted to make a solution containing 4ug per lml, which is determined by UV-Vis spectrophotometry (General 0401), there is a maximum absorption at a wavelength of 244Nm and a minimum absorption at a wavelength of 227nm.
  3. The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 993).
  4. This product shows the identification reaction of organic fluoride (General rule 0301).
Last Update：2022-01-01 13:40:23

ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate - Exam

Authoritative Data Verified Data

clarity and color of acetic acid solution

take this product 0.lg, add acetic acid 10ml after dissolution, the solution should be clear and colorless.

Related substances

The product was taken, and the mobile phase was added to make a test solution containing 1.0 mg per 1 ml and a control solution containing 10ug per 1 ml. Test according to high performance liquid chromatography (General 0512). Silica gel bonded with eighteen alkyl silane was used as filler; Dilute phosphoric acid solution (2.0 of water was taken, pH was adjusted to with phosphoric acid)-methanol-tetrahydrofuran (80:13:7) was used as mobile phase; the detection wavelength was 230nm. The number of theoretical plates shall not be less than 3000 based on the flumazenil peak. 20ul of control solution and 20ul of test solution were respectively injected into human liquid chromatograph, and the chromatogram was recorded to 3 times of the retention time of principal component peak. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than 0.2 times (0.2%) of the area of the main peak of the control solution, the sum of each impurity peak area shall not be greater than 0.5 times (0.5%) of the main peak area of the control solution.

loss on drying

take this product, dry to constant weight at 105°C, weight loss shall not exceed 0.2% (General rule 0831).

ignition residue

take 1.0g of this product, put it in a platinum crucible, and check it according to law (General rule 0841). The remaining residue shall not exceed 0.1%.

Heavy metals

The residue left under the item of taking the ignition residue shall not contain more than 20 parts per million of heavy metal when examined by law (General rule 0821, Law II).

Last Update：2022-01-01 13:40:23

ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate - Content determination

Authoritative Data Verified Data

take this product about 0.25g, precision weighing, add glacial acetic acid 30ml and acetic anhydride 20ml dissolved, according to the potential titration method (General rule 0701), with perchloric acid titration solution (O. 1 mol/L) titration, and the results of the titration were corrected with a blank test. Each 1 ml of perchloric acid titration solution (0.1 mol/L) corresponds to 30.33mg of C15H14FN3O3.

Last Update：2022-01-01 13:40:24

ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate - Category

Authoritative Data Verified Data

benzodiazepine antagonists.

Last Update：2022-01-01 13:40:24

ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate - Storage

Authoritative Data Verified Data

light shielding, sealed storage.

Last Update：2022-01-01 13:40:25

ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate - Flumazenil Injection

Authoritative Data Verified Data

This product is a sterile aqueous solution of flumazenil. The fluorine-containing Masini (C15H14FN3O3) shall be 90.0%-110.0% of the labeled amount.

trait

This product is a clear colorless liquid.

identification

In the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the control solution.

examination

  • the pH value should be 3.5 to 4.2 (General 0631).
  • Related substances this product was taken as a test solution; An appropriate amount was taken in a precise amount, and water was added for quantitative dilution to prepare a solution containing about 1 ton of fluorine-containing Masini per 1 ml, which was used as a control solution. The determination was carried out according to the method for related substances of clemazini. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than the area of the main peak of the control solution (1.0%), the sum of each impurity peak area shall not be greater than 2 times (2.0%) of the main peak area of the control solution.
  • bacterial endotoxin take this product, according to the law inspection (General 1143), the amount of endotoxin per 1 mg flumazenil should be less than 25EU.
  • others should comply with the relevant provisions under injection (General 0102).

Content determination

  • measured by high performance liquid chromatography (General 0512).
  • chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica gel as filler; Dilute phosphoric acid solution (1000ml of water, adjusted to pH 2.0 with phosphoric acid)-methanol-tetrahydrofuran (80:13:7) as mobile phase; Detection wavelength, 230nm. The number of theoretical plates shall not be less than 3000 based on the flumazenil peak.
  • determination of this product, as a test solution, the precise amount of 20u1 injection of human liquid chromatography, record the chromatogram; Another flumazenil reference product about 20mg, precise weighing, in a 200ml measuring flask, add 20ml of methanol, shake to dissolve, dilute to the scale with water, shake well, and measure with the same method. According to the external standard method to calculate the peak area, that is.

category

Same as flumazenil.

specification

(l)2ml:0.2mg (2)5ml:0.5mg (3)10ml:1.Omg

storage

protected from light and sealed.

Last Update：2022-01-01 13:40:25

ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate - Reference Information

NIST chemical information information provided by: webbook.nist.gov (external link)
Application Clinical discontinuation of benzodiazepine? Induction and maintenance of general anesthesia; Reversal of benzodiazepine? Poisoning caused by overdose; Used for benzodiazepine? Diagnosis of poisoning; Used for the treatment of hepatic coma.
Use The first benzodiazepine antagonist, it is used to combat the sedative effect and disorientation after overdose of benzodiazepine drugs, and has anticonvulsant activity and antiepileptic effect, it can also be used for the recovery period after halothane anesthesia and encephalopathy due to cirrhosis caused by alcoholism, as a diagnostic drug for unexplained loss of consciousness, to identify benzodiazepine and other drug poisoning or brain damage.
stimulant for central nervous system.
drug substance
production method Method 1: oxidation of 5-fluoroisatin in glacial acetic acid and concentrated sulfuric acid with 30% hydrogen peroxide, 6-fluoroisatoic anhydride was obtained as a yellow solid in 82% yield. Then, it was reacted with sarcosine (I. E., N-Methylglycine) in dimethyl sulfoxide at 100 ° C. To obtain compound (I) in 80% yield. Again in chloroform, in the presence of N,N-dimethylaniline, and phosphorus oxychloride reflux. The compound (II) obtained by chlorination was treated and reacted with ethyl cyanoacetate in dimethylformamide in the presence of sodium tert-butoxide to obtain flumazenil with a yield of 40% and a melting point of 200-203 °c. Method 2: 4-fluoro-2-(N-carboxyamino) benzoic acid and N-Methylglycine are cyclized to form compound (III), which is then cyclized with ethyl 2-cyanoacetate to obtain flumazenil.
Last Update：2024-04-10 22:29:15
ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
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CAS: 78755-81-4
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Hefei TNJ Chemical Industry Co.,Ltd.
Product Name: Flumazenil Request for quotation
CAS: 78755-81-4
Tel: 0086-551-65418684
Email: sales@tnjchem.com
　　　　 info@tnjchem.com
Mobile: 0086 189 4982 3763
QQ: 2881500840 Click to send a QQ message
Wechat: 0086 189 4982 3763
WhatsApp: 0086 189 4982 3763
Product List: View Catalog
Shanghai Yuanye Bio-Technology Co., Ltd.
Multiple SpecificationsSpot supply
Product Name: Flumazenil Visit Supplier Webpage Request for quotation
CAS: 78755-81-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
Wechat: 18301782025
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ethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
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