BROTIZOLAM Property

Melting point:

204-206?C

Boiling point:

561.3±60.0 °C(Predicted)

Density 

1.6265 (estimate)

storage temp. 

-20°C Freezer

solubility 

Practically insoluble in water, sparingly soluble or slightly soluble in methanol, slightly soluble in ethanol (96 per cent).

pka

2.01±0.40(Predicted)

form 

A crystalline solid

Safety

Toxicity

LD50 in mice, rats (mg/kg): >10000, >10000 orally; 920, 1000 i.p. (Hewett)

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H336May cause drowsiness or dizziness

H361Suspected of damaging fertility or the unborn child

H362May cause harm to breast-fed children

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P263Avoid contact during pregnancy/while nursing.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

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

P271Use only outdoors or in a well-ventilated area.

P281Use personal protective equipment as required.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P308+P313IF exposed or concerned: Get medical advice/attention.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

BROTIZOLAM Chemical Properties,Usage,Production

Description

Brotizolam is a hypnotic/sedative approximately 60-100 times more potent than flurazepam. As with other short-acting, annulated benzodiazepines (e.g., triazolam), cited advantages include lack of adverse effects on sleep and performance after arousal.

Chemical Properties

Tan Solid

Originator

Boehringer Ingelheim (W. Germany)

Uses

A hypnotic and a sedative, also used in veterinary medicine as an appetite stimulant

Definition

ChEBI: Brotizolam is an organic molecular entity.

Manufacturing Process

(a) 11.5 g of 7-bromo-5-(o-chlorophenyl)-3H-[2,3e]-thieno-1,4-diazepin-2- one (see German Patent 2,221,623), were heated at 55° to 60°C with 100 cc of absolute pyridine and 6.5 g of phosphorus pentasulfide for 4 hours while stirring. The mixture was allowed to cool and was then poured into 100 cc of saturated ice-cold NaCl solution. The precipitate was collected by suction filtration, washed with water, dissolved in 100 cc of methylene chloride, the solution was dried and evaporated, and the residue was treated with a little methylene chloride. After suction filtration, 6 g of brown crystalline 7-bromo- 5-(o-chlorophenyl)-3H-[2,3e]-thieno-1,4-diazepine-2-thione, melting point 214°C (decomposition) were obtained.
(b) 6.0 g of this compound were suspended in 100 cc of tetrahydrofuran, and the suspension was stirred at room temperature with 1.2 g of hydrazine hydrate for 20 minutes. After evaporation to about 10 cc, 20 cc of ether were added, and the crystals were collected by suction filtration. Yield: 5.2 g of 7- bromo-5-(o-chlorophenyl)-2-hydrazino-3H-[2,3e]-thieno-1,4-diazepine, melting point about 300°C (decomposition).
(c) 5.2 g of this compound were suspended in 50 cc of orthotriethyl acetate, and the suspension was heated to 80°C. After about 30 minutes a clear solution was first formed from which later colorless crystals separated out. The mixture was allowed to cool, and the crystals were collected by suction filtration and washed with ether. Yield: 5 g of the compound, melting point 211° to 213°C.

brand name

Lendorm (Boehringer Ingelheim);LENDORMIN.

Therapeutic Function

Psychotropic