CLOTIAZEPAM Property

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)

Safety

Toxicity

LD50 in mice (mg/kg): 440 i.p., 636 orally (Nakanishi)

Hazard and Precautionary Statements (GHS)

CLOTIAZEPAM Chemical Properties,Usage,Production

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