ZOPICLONE

PRODUCT IDENTIFICATION
CAS NO. 43200-80-2

ZOPICLONE 

EINECS NO. 256-138-9
FORMULA C17H17ClN6O3
MOL WT. 388.81

H.S. CODE

  

TOXICITY

  
SYNONYMS Amoban; Amovane; Imovane; Zopiclona;
Zopiclone; Zopiclonum; (+-)-Zopiclone; 4-Methyl-1-piperazinecarboxylic acid 6-(5-chloro-2-pyridyl)-6,7-dihydro-7 -hydroxy-5H-pyrrolo(3,4-b)pyrazin-5-one ester; 1-Piperazinecarboxylic acid, 4-methyl-, 6-(5-chloro-2-pyridinyl)-6,7-dihydro-7-oxo-5H- pyrrolo(3,4-b)pyrazin-5-yl ester; 6-(5-Chloro-2-pyridinyl)-6,7-dihydro-7-oxo-5H-pyrrolo(3,4- b)pyrazin-5-yl 4-methyl- piperazine-1-carboxylate
DERIVATION

 

CLASSIFICATION

  

PHYSICAL AND CHEMICAL PROPERTIES

PHYSICAL STATE slightly yellowish crystalline powder
MELTING POINT 177 C (Decomposes)
BOILING POINT

 

RELATIVE DENSITY  
SOLUBILITY IN WATER

Insoluble

pH  
VAPOR DENSITY

 

REFRACTIVE INDEX

 

NFPA RATINGS

  

AUTOIGNITION

 

FLASH POINT

 

STABILITY Stable under normal conditions.

GENERAL DESCRIPTION & APPLICATIONS
Zopiclone is a hypnotic agent. Molecularly It is a pyrrolopyrazine derivative of cyclopyrrolone family. Cyclopyrrolone structure is not related to benzodiazepine which is a common molecular structure (a fused structure between the benzene and diazepine ring) acting as depressants of the central nervous system (antianxiety, sedative, hypnotic, amnestic, anticonvulsant, and muscle relaxing). Though cyclopyrrolone are distinct from benzodiazepines in structure, they have similar activity to that of benzodiazepines. Zopiclone was introduced  with the benefit of less addictive potential than benzodiazepine drugs. But some reports doubt on the claim.  Zopiclone also has some barbiturate like pharmacological properties. Other cyclopyrrolones include pagoclone, pazinaclone, suriclone and suproclone.

Zopiclone is a sedative-hypnotic used in the short-term treatment of insomnia (difficulties with falling asleep). Zopiclone possesses a chiral center but is commercially marketed as a racemic of two stereoisomers, only (S)-configuration is active. Eszopiclone is the S(+)-enantiomer of racemic zopiclone. The chemical name of zopiclone is 6-(5-chloro-2-pyridinyl)- 6,7-dihydro- 7-oxo-5H-pyrrolo(3,4- b)pyrazin-5-yl 4-methyl- piperazine-1- carboxylate. It is a white to yellowish crystalline powder; insoluble in water and very slightly soluble in ethanol. Zopiclone positively modulates GABAa receptors by selectively binding to a particular part of a receptor in the brain called GABA receptors. This causes the release of a chemical called GABA (gamma amino butyric acid) which is a major inhibitory chemical in the brain which is responsible for causing sleepiness and controlling anxiety and fits. This type of drugs include Z-drugs (zopiclone, eszopiclone, zolpidem, and zaleplon), allopregnanolone, barbiturates, flunitrazepam, diazepam, alprazolam, and abecarnil. Increasing GABA release by these drugs helps falling sleep, decreasing anxiety and relaxing the muscles.

SEDATIVE / HYPNOTIC DRUGS

  • Barbiturates
    • Amobarbital Sodium (CAS RN: 64-43-7)
    • Aprobarbital (CAS RN: 77-02-1)
    • Butabarbital (CAS RN: 125-40-6)
    • Butalbital (CAS RN: 77-26-9)
    • Hexobarbital (CAS RN: 56-29-1)
    • Phenobarbital (CAS RN: 50-06-6)
    • Seconal (CAS RN: 76-73-3)
    • Talbutal (CAS RN: 115-44-6)
    • Thiopental (CAS RN: 76-75-5)
  • Nonbarbiturate, Nonbenzodiazepine
    • Chlormethiazole
    • Acetylcarbromal
    • Dexmedetomidine (CAS RN: 113775-47-6)
    • Glutethimide (CAS RN: 77-21-4)
    • Zalepon
    • Zopiclone (CAS RN: 43200-80-2)
    • Triclofos (CAS RN: 306-52-5)
    • Chloral Hydrate (302-17-0)
    • Promethazine (CAS RN: 60-87-7)
    • Diphenhydramine (CAS RN: 58-73-1)
    • Zolpidem (CAS RN: 82626-48-0)
    • Buspirone (CAS RN: 36505-84-7)
    • Ethchlorvynol (CAS RN: 113-18-8)
    • Ethinamate (CAS RN: 126-52-3)
    • Meprobamate (CAS RN: 57-53-4)
    • Methaqualone (CAS RN: 72-44-6)
    • Dimerin (CAS RN: 125-64-4)
    • Paraldehyde (CAS RN: 123-63-7)
    • Thalidomide (CAS RN: 50-35-1)
SALES SPECIFICATION

APPEARANCE

 slightly yellowish crystalline powder

IDENTIFICATION

to pass test A, B, C

ASSAY

98.5 - 100.5%
RELATED SUBSTANCES

0.5% max

HEAVY METALS

20ppm max
PROPANOL

0.7% max

SULFATE

0.1% max
SPECIFIC ROTATION -0.05° ~ +0.05°
TRANSPORTATION
PACKING
 
HAZARD CLASS  
UN NO.

 

OTHER INFORMATION
Hazard Symbols: XN, Risk Phrases: 20/21/22-36/37/38-62, Safety Phrases: 26-36
PRICES

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