308242-62-8

Basic information

• Product Name: CNS 7056
• Synonyms: CNS 7056;ReMiMazolaM;methyl 3-[(4S)-8-bromo-1-methyl-6-pyridin-2-yl-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]propanoate CNS-7056 Remimazolam;Remimazolam Tosylate;Vibegron;Methyl 3-[(4S)-8-bromo-1-methyl-6-(2-pyridyl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]propanoate
• CAS NO: 308242-62-8
• Molecular Formula: C₂₁H₁₉BrN₄O₂
• Molecular Weight: 439.30516
• Product Categories: API
• Mol File: 308242-62-8.mol
• Article Data: 5

Chemical Properties

• Boiling Point: 583.5±60.0 °C(Predicted)
• Appearance: /
• Density: 1.48±0.1 g/cm3(Predicted)
• PKA: 5.58±0.60(Predicted)
• CAS DataBase Reference: CNS 7056(CAS DataBase Reference)
• NIST Chemistry Reference: CNS 7056(308242-62-8)
• EPA Substance Registry System: CNS 7056(308242-62-8)

Safety Data

• Hazardous Substances Data: 308242-62-8(Hazardous Substances Data)

Upstream product

• 45214-91-3 (2S)-2-[(tert-butoxy)carbonylamino]-4-(methoxycarbonyl)butanoic acid 
• 1275616-59-5 3-[(S)-7-bromo-2-((R)-2-hydroxypropylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]propionic acid methyl ester 
• 1275616-60-8 (S)-methyl 3-(7-bromo-2-((dimorpholinophosphoryl)oxy)-5-(pyridin-2-yl)-3H-benzo[e][1,4]diazepin-3-yl)propanoate 
• 1275616-58-4 C₁₈H₁₈BrN₃O₄*ClH 
• 1275616-57-3 C₂₃H₂₆BrN₃O₆ 
• 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 
• 1563-56-0 2-amino-5-bromobenzoyl pyridine 
• 308243-54-1 C₂₁H₂₃BrN₄O₃ 

Downstream Products

• 1001415-66-2 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]propionic acid methyl ester benzenesulfonate 

Relevant articles and documents

PROCESS FOR THE PREPARATION OF REMIMAZOLAM AND SOLID STATE FORMS OF REMIMAZOLAM SALTS

The present disclosure relates to novel processes for the preparation of short acting benzodiazepines as well as to novel intermediates in this process. More particularly the disclosure relates to processes and intermediates for preparation of Methyl 3-[(4S)-8-bromo-1-methyl-6-(pyridin-2-yl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]propanoate, commonly known as Remimazolam. The present disclosure also relates to solid state forms of Remimazolam salts, processes for the preparation thereof, pharmaceutical formulations / compositions thereof, and methods of use thereof.

PROCESS FOR PREPARING 3-[(4S)-8-BROMO-1-METHYL-6-(2-PYRIDINYL)-4H-IMIDAZOL[1,2-A][1,4]BENZODIAZEPINE-4-YL]PROPIONIC ACID METHYL ESTER OR THE BENZENE SULFONATE SALT THEREOF, AND COMPOUNDS USEFUL IN THAT PROCESS

The invention concerns a new process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]-propionic acid methyl ester 3-[(4S)-8-bromo-1 -methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]propioni

SHORT-ACTING BENZODIAZEPINES

It has now been found that compounds of the present invention as described in Benzodiazepine derivatives of Formula (I) containing a carboxylic ester moiety and thereby capable of being inactivated by nonspecific tissue esterases in an organ-independent elimination mechanism and thereby providing a more predictable and reproducible pharmacodynamic profile. The compounds of the present invention are suitable for therapeutic purposes, including sedative-hypnotic, anxiolytic, muscle relaxant and anticonvulsant purposes and are useful to be administered intravenously in the following clinical settings: preoperative sedation, anxiolysis, and amnestic use for perioperative events; conscious sedation during short diagnostic, operative or endoscopic procedures; as a component for the induction and maintenance of general anesthesia, prior and/or concomitant to the administration of other anesthetic agents; ICU sedation.