ZOTEPINE Property

Melting point:

90-91°

Boiling point:

478.4±45.0 °C(Predicted)

Density 

1.0675 (rough estimate)

refractive index 

1.6100 (estimate)

storage temp. 

Store at RT

solubility 

DMSO: ≥20mg/mL

pka

8.72±0.28(Predicted)

form 

powder

color 

white to off-white

Safety

Hazard Codes 

T

Risk Statements 

25-50/53

Safety Statements 

45-60-61

RIDADR 

UN 2811 6.1 / PGIII

WGK Germany 

3

Toxicity

LD50 in male mice, rats (mg/kg): 108, 458 orally; 43.3, 39.7 i.v.; 40.0, 97.0 i.p.; 84.9, 2080 s.c. (Fukuhara)

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H301Toxic if swalloed

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P273Avoid release to the environment.

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

P391Collect spillage. Hazardous to the aquatic environment

P405Store locked up.

ZOTEPINE Chemical Properties,Usage,Production

Chemical Properties

White to off white crystalline powder

Originator

Lodopin,Fujisawa Pharmaceutical,Japan,1982

Uses

antipsychotic;Dopamine D2/serotonin 5-HT2 antagonist

Definition

ChEBI: Zotepine is a dibenzothiepine and a tertiary amino compound. It has a role as an alpha-adrenergic drug, a serotonergic drug and a second generation antipsychotic.

Manufacturing Process

A suspension of 30 g of sodium hydride in benzene (30 ml) was added dropwise to 52 g of 8-chlorodibenzo[b,f]thiepin-10(11H)-one dissolved in dimethylformamide (800 ml), and the mixture was heated at 100°C for 2 hours. To this, there were added 68 g of 2-dimethylaminoethyl chloride, and the mixture was heated at 60°C for 39 hours. The reaction mixture, after cooled, was poured into ice-water, and the solution was extracted with ethyl acetate. The ethyl acetate layer, after washed with water, was extracted with 10% hydrochloric acid, when oil was precipitated. The aqueous layer, in which oil was precipitated, was washed with ether, made neutral with concentrated sodium hydroxide solution and then extracted with ethyl acetate. The ethyl acetate layer was washed with water, dried over magnesium sulfate, and concentrated to give oil, which was allowed to stand to provide solid. The solid was washed with petroleum ether and recrystallized from cyclohexane to yield 42.5 g of 8-chloro-10-(2-dimethylaminoethyl)-oxydibenzo[b,f]thiepin as crystals, melting point 90°C to 91°C. Maleate as colorless needle, melting point 204°C to 204.5°C.

Therapeutic Function

Tranquilizer