ALPHAPRODINE HYDROCHLORIDE CII (250 MG) Property

Melting point:

220-221°

solubility 

Methanol (Slightly)

form 

Solid

color 

White to Off-White

Stability:

Hygroscopic

Safety

Hazard Codes 

F,T

Risk Statements 

11-23/24/25

Safety Statements 

16-22-36/37/39-45

Toxicity

LD50 in mice: 54 mg/kg i.v., 73 mg/kg i.p.; in rats: 22 mg/kg i.p. (Gruber)

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H301Toxic if swalloed

H311Toxic in contact with skin

H330Fatal if inhaled

Precautionary statements

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

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.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P284Wear respiratory protection.

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

P302+P352IF ON SKIN: wash with plenty of soap and water.

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

P310Immediately call a POISON CENTER or doctor/physician.

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

P320Specific treatment is urgent (see … on this label).

P321Specific treatment (see … on this label).

P322Specific measures (see …on this label).

P330Rinse mouth.

P361Remove/Take off immediately all contaminated clothing.

P363Wash contaminated clothing before reuse.

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

P405Store locked up.

P501Dispose of contents/container to..…

ALPHAPRODINE HYDROCHLORIDE CII (250 MG) Chemical Properties,Usage,Production

Originator

Nisentil ,Roche ,US ,1949

Uses

Analgesic (narcotic). Controlled substance (opiates).

Manufacturing Process

In a round-bottom flask provided with stirrer, dropping funnel, condenser and a gas outlet for keeping the system under nitrogen, 200 cc of dry ether is placed and 4.6 grams of lithium cut into thin strips is added. 52 grams of bromobenzene in 50 cc of dry ether are added dropwise and after addition, the mixture is refluxed for 2 hours. This procedure results in the formation of phenyl-lithium. Other aryl-lithium compounds can be prepared in a similar manner by reacting lithium metal or a lithium compound capable of transferring lithium and a compound having an exchangeable halogen group as, for example, bromonaphthalene.
The solution of phenyl-lithium is cooled to -20°C and to this a solution of 12.7 grams of 1,3-dimethyl-4-piperidone, prepared according to the method of Howton, J. Org. Chem. 10, 277 (1945), in ether is added dropwise with stirring. After the addition, the stirring is continued for a further 2 hours at - 20°C. The lithium complex, 1,3-dimethyl-4-phenyl-4-oxylithium piperidine, which forms is soluble in the ether and can be recovered there from. To prepare the piperidinol, the lithium complex, while in the reaction mixture is decomposed by the addition of an ice and hydrochloric acid mixture. The acidified layer is separated, basified and extracted with ether. After drying the ether solution and removing the solvent, the residue on distillation in vacuum distills chiefly at 155°C/10 mm, yielding the product, 1,3-dimethyl-4-phenyl- 4-hydroxypiperidine, which, on crystallization from n-hexane melts at 102°C. On treatment with propionic anhydride catalyzed with a trace of sulfuric acid,1,3-dimethyl-4-propionoxy-4-phenylpiperidine is attained. The latter compound can be converted into the hydrochloride salt by reaction with hydrogen chloride. This salt after crystallization from acetone has a melting point of 209°C.

brand name

Nisentil (Hoffmann-LaRoche).

Therapeutic Function

Narcotic analgesic