BENACTYZINE HYDROCHLORIDE Property

Melting point:

177-179 °C(lit.)

storage temp. 

Keep in dark place,Sealed in dry,Room Temperature

solubility 

DMSO (Slightly, Heated), Methanol (Slightly)

form 

Solid

color 

Crystals from Me2CO

Merck 

14,1029

CAS DataBase Reference

57-37-4(CAS DataBase Reference)

EPA Substance Registry System

Benzeneacetic acid, .alpha.-hydroxy-.alpha.-phenyl-, 2-(diethylamino)ethyl ester, hydrochloride (57-37-4)

Safety

Hazard Codes 

T

Risk Statements 

23/24/25

Safety Statements 

36/37/39-45

RIDADR 

UN 2811 6.1/PG 3

WGK Germany 

3

RTECS 

DD2800000

HS Code 

2922.50.4000

HazardClass 

6.1(b)

PackingGroup 

III

Toxicity

LD50 orl-rat: 184 mg/kg TXAPA9 1,42,59

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H301Toxic if swalloed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

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

P405Store locked up.

P501Dispose of contents/container to..…

BENACTYZINE HYDROCHLORIDE Chemical Properties,Usage,Production

Originator

Suavitil,Merck Sharp and Dohme,US,1957

Uses

Benactyzine Hydrochloride is an antagonist of acetylcholine in the central and peripheral nervous system. Benactyzine Hydrochloride is used as an antispasmodic.

Manufacturing Process

114 parts of ethyl benzilate, 175 parts of β-diethylaminoethanol and 0.2 part of metallic sodium were placed in a flask attached to a total-reflux variable take-off fractionating column. The pressure was reduced to 100 mm and heat was applied by an oil bath the temperature of which was slowly raised to 90°C. During three hours of heating 17 parts of ethanol distilled (35.5°C). When the distillation of the ethanol became slow, the bath temperature was raised to 120°C. When the vapor temperature indicated distillation of the amino alcohol the take off valve was closed and the mixture was refluxed for one hour. At the end of this period the vapor temperature had dropped and two more parts of ethanol were distilled, The remaining aminoalcohol was slowly distilled for three hours. The pressure was then reduced to 20 mm and the remainder of the aminoalcohol distilled at 66°C. During the reaction the color of the solution changed from yellow to deep red. The residue was dissolved in 500 parts of ether, washed once with dilute brine, and three times with water, dried over sodium sulfate and finally dried over calcium sulfate. 500 parts of a saturated solution of HCl in absolute ether was added and the resulting precipitate filtered. Dry HCl gas was passed into the filtrate to a slight excess and the precipitate again filtered. The combined precipitates were washed with cold acetone. The 106 parts of product was purified by recrystallization from acetone as fine white crystals which melt at 177°- 178°C.

Therapeutic Function

Tranquilizer; Anticholinergic

Safety Profile

Poison by ingestion, intraperitoneal, subcutaneous, intradermal, and intravenous routes. Human systemic effects by ingestion of very small amounts: toxic psychosis. Experimental reproductive effects. When heated to decomposition it emits very toxic fumes of NO, and HCl