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????? ??
- ???
- 25°C
- ?? ?
- bp0.45 125-135°; bp3 173-175°
- ??
- 1.1388 (rough estimate)
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- nD25 1.5842 (also reported as 1.5835)
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- Refrigerator, under inert atmosphere
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- DMSO(??), ???(??)? ???
- ??? ??
- ??
- ?? ?? (pKa)
- pKa 3.02 ± 0.05;8.24± 0.11(H2O,t undefined,I=0.30(NaCl)) (Uncertain)
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- ??~???
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- 601.2mg/L(30℃)
- Henry's Law Constant
- 3.6×101 mol/(m3Pa) at 25℃, HSDB (2015)
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- ?? ? ???? ?? (GHS)
| ????(UN No.) | 1851 | ||
|---|---|---|---|
| ?? ?? | 6.1(b) | ||
| ???? | III | ||
| ?? ?? ??? | 91-80-5(Hazardous Substances Data) | ||
| ?? | LD50 in mice, guinea pigs (mg/kg): 182.2 ±12.8, 374.9 ±34.5 orally; in mice (mg/kg): 19.85 ±0.69 i.v. (Lee) |
| ????(GHS): |
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| ?? ?: | Danger | ||||||||||||||||
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????? C??? ??, ??, ??
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colourless liquid??
Methapyrilene is an intermediate in the synthesis of Methapyrilene Hydrochloride (M259970). Methapyrilene is used as antihistaminic agent.??
ChEBI: A member of the class of ethylenediamine derivatives that is ethylenediamine in which one of the nitrogens is substituted by two methyl groups, and the other nitrogen is substituted by a 2-pyridyl group and a (2-thienyl)methyl group.World Health Organization (WHO)
Methapyrilene, an antihistamine with moderate sedative activity, was introduced in 1947 for the treatment of various allergic conditions and was subsequently incorporated in many over-the-counter sleeping aids. In the early 1970s it was identified as a carcinogen in rats and, although there was no direct evidence that it constitutes a health hazard to man, it was withdrawn in many countries. (Reference: (WHODI) WHO Drug Information, 2, 4, 1979)?? ??
Clear colorless liquid.?? ???
An amine, organosulfide. Organosulfides are incompatible with acids, diazo and azo compounds, halocarbons, isocyanates, aldehydes, alkali metals, nitrides, hydrides, and other strong reducing agents. Reactions with these materials generate heat and in many cases hydrogen gas. Many of these compounds may liberate hydrogen sulfide upon decomposition or reaction with an acid. Amines are chemical bases. They neutralize acids to form salts plus water. These acid-base reactions are exothermic. The amount of heat that is evolved per mole of amine in a neutralization is largely independent of the strength of the amine as a base. Amines may be incompatible with isocyanates, halogenated organics, peroxides, phenols (acidic), epoxides, anhydrides, and acid halides. Flammable gaseous hydrogen is generated by amines in combination with strong reducing agents, such as hydrides.????
ACUTE/CHRONIC HAZARDS: METHAPYRILENE is highly toxic by ingestion.????
Flash point data for METHAPYRILENE are not available, but METHAPYRILENE is probably combustible.?? ?? ??
When methaphenilene is incubated with rat liver microsomes, it is metabolized via N-oxide formation and N-dealkylation which includes removal of the dimethylamino moiety, the thiophenylmethyl moiety of methaphenilene, and the benzyl moiety of pyribenzamine.????? ?? ?? ? ???
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2-??????
N-(2-?????)???-2-??
2-??????
2-(Chloromethyl)thiophene
2-Chloroethyldimethylamine
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???( 25)?? ??
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