1001415-66-2

Basic information

• Product Name: Remimazolam (benzenesulfonate)
• Synonyms: Remimazolam (benzenesulfonate);Remimazolam benzenesulfonat
• CAS NO: 1001415-66-2
• Molecular Formula: C₆H₆O₃S*C₂₁H₁₉BrN₄O₂
• Molecular Weight: 597.4802
• Mol File: 1001415-66-2.mol
• Article Data: 4

Chemical Properties

• Appearance: /
• CAS DataBase Reference: Remimazolam (benzenesulfonate)(CAS DataBase Reference)
• NIST Chemistry Reference: Remimazolam (benzenesulfonate)(1001415-66-2)
• EPA Substance Registry System: Remimazolam (benzenesulfonate)(1001415-66-2)

Safety Data

• Hazardous Substances Data: 1001415-66-2(Hazardous Substances Data)

Usage

General Description

Remimazolam (benzenesulfonate) is a water-soluble benzodiazepine derivative that is being developed as a short-acting sedative for use in procedural sedation and general anesthesia. It acts on the gamma-aminobutyric acid (GABA) receptor in the brain, producing sedative, anxiolytic, amnestic, and muscle relaxant effects. Its rapid onset and short duration of action make it an attractive option for use in medical procedures, as it allows for quick recovery and discharge of the patient. Remimazolam has shown promising results in clinical trials for sedation during colonoscopy and other minor surgical procedures, and it is being further studied for its potential applications in anesthesia.

Upstream product

• 308242-62-8 Remimazolam 
• 98-11-3 benzenesulfonic acid 
• 1275616-61-9 3-[(S)-7-bromo-2-(2-oxopropylamino)-5-pyridin-2-yl-3H-1,4-benzodiazepin-3-yl]propionic acid methyl ester 
• 308242-23-1 (3S)-3-(7-bromo-2-oxo-5-pyridin-2-yl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)propionic acid methyl ester 
• 4652-65-7 (S)-2-Benzyloxycarbonylamino-pentanedioic acid 5-methyl ester 
• 1499-55-4 L-glutamic acid 5-methyl ester 

Relevant articles and documents

Preparation method of benzodiazepine drugs

The invention discloses a preparation method of benzodiazepine drugs. The method comprises the following steps: (1) reacting an intermediate shown as a formula II with dimorpholinophosphoryl chloride(BMPC) in the presence of lithium diisopropylamide to generate an active intermediate, adding 1-amino 2-propanol of raceme, and treating after the reaction is ended, recrystallizing methyl tert-butylether to obtain an intermediate refined product shown in a formula III; and (2) oxidizing the intermediate refined product shown in the formula III obtained in the step (1), and performing cyclizationand salification by using benzenesulfonic acid to separate out a compound shown in a formula I. Compared with the prior art, the method is easy and convenient to operate, low in cost, high in yield and suitable for industrial production.

OXIDATION REACTION EXCELLENT IN CONVERSION RATE

A process for preparing 3-[(S)-7-bromo-2-(2-oxo-propylamino)-5-pyridin-2-yl-3H-1,4,-benzodiazepin-3-yl]propionic acid methyl ester at a high conversion rate with good reproducibility by oxidizing 3-[(S)-7-bromo-2-(2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]propionic acid methyl ester in the presence of an oxidation catalyst is provided by defining the ammonium ion content of 3-[(S)-7-bromo-2-(2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]propionic acid methyl ester.