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CLOTIAZEPAM

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CLOTIAZEPAM Basic information

Product Name:
CLOTIAZEPAM
Synonyms:
  • CLOTIAZEPAM
  • 2H-Thieno(2,3-e)(1,4)diazepin-2-one, 1,3-dihydro-5-(o-chlorophenyl)-7-ethyl-1-methyl-
  • 2H-Thieno(2,3e)(1,4)-diazepin-2-one, 5-(o-chlorophenyl)-7-ethyl-1,3-dihydro-1-methyl-
  • 2h-thieno(2,3-e)(1,4)diazepin-2-one,1,3-dihydro-5-(o-chlorophenyl)-7-ethyl-1-m
  • 2h-thieno(2,3e)(1,4)-diazepin-2-one,5-(o-chlorophenyl)-7-ethyl-1,3-dihydro-1
  • 2H-Thieno[2,3-e]-1,4-diazepin-2-one, 5-(2-chlorophenyl)-7-ethyl-1,3-dihydro-1-methyl-
  • 2H-Thieno[2,3-E]-1,4-diazepine-2-one, 5-(2-chlorophenyl)-7-ethyl-1,3-dihydro-1-methyl-
  • 5-(2-chlorophenyl)-7-ethyl-1-methyl-1,3-dihydro-2h-thieno(2,3-e)(1,4)diazepi
CAS:
33671-46-4
MF:
C16H15ClN2OS
MW:
318.82
EINECS:
251-627-3
Product Categories:
  • Agonist
  • Aromatics
  • Heterocycles
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Sulfur & Selenium Compounds
Mol File:
33671-46-4.mol
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CLOTIAZEPAM Chemical Properties

Melting point:
105-106°
Boiling point:
523.7±50.0 °C(Predicted)
Density 
1.1625 (rough estimate)
refractive index 
1.6100 (estimate)
solubility 
DMF: 15 mg/ml; DMSO: 15 mg/ml; DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
form 
A crystalline solid
pka
2.36±0.20(Predicted)
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Safety Information

Toxicity
LD50 in mice (mg/kg): 440 i.p., 636 orally (Nakanishi)
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CLOTIAZEPAM Usage And Synthesis

Chemical Properties

Off-White Solid

Originator

Rize,Yoshitomi,Japan,1979

Uses

A thienodiazepine derivative that possesses anxiolytic, skeletal muscle relaxant anticonvulsant, sedative properties as well as contributing to siginificant increase stage 2 NREM sleep. It binds to be nzodiazepine site of the GABAA receptor where it acts as a full agonist resulting in enhanced GABA inhibitory effect at the GABAA receptor. Controlled Substance.

Definition

ChEBI: Clotiazepam is an organic molecular entity.

Manufacturing Process

To a solution of 10 g of 2-N-methylaminoacetamido-3-o-chlorobenzoyl-5-ethylthiophene in 50 ml of pyridine are added 20 ml of benzene and 1.9 g of acetic acid. The resulting mixture is refluxed with stirring for 10 hours in a flask provided with a water-removing adaptor. The reaction mixture is concentrated, and the residue is extracted with chloroform. The chloroform layer is washed with water and then with a sodium hydrogen carbonate solution, then dried over magnesium sulfate. The chloroform is distilled off under reduced pressure, and toluene is added to the residue. Thus is precipitated white crystalline-5-o-chlorophenyl-7-ethyl-1-methyl-1,2-dihydro- 3H-thieno-[2,3-e][1,4]diazepin-2-one, MP 105°C to 106°C.

Therapeutic Function

Tranquilizer

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