English name: Praziquantel
English alias: embay8440; biltricide; Prazinon; Azinox; Cysticide;
CAS Number: 55268-74-1
Molecular formula: C19H24N2O2
Molecular weight: 312.40600
Exact mass: 312.18400
PSA: 40.62000
LogP: 2.41070
physicochemical properties
Appearance and properties: white or almost white crystalline powder
Density: 1.22 g/cm3
Melting point: 136-142ºC
Boiling point: 544.1ºCat 760 mmHg
Flash point: 254.6ºC
Stability: stable under normal temperature and pressure
Storage conditions: ventilated and dry at low temperature
Security Information
Customs code: 2933790090
WGK Germany: 1
Hazard category code: R11
Safety Instructions: S16; S26; S36/37/39; S45
RTECS number: UQ4150000
Dangerous Goods Sign: F; C [1]
production method
Using phenethylamine as raw material, after acylation with chloroacetyl chloride, amination reaction with potassium phthalamide to introduce amino group, and cyclization under the action of phosphorus oxychloride to obtain 3,4-dihydroisoquinoline The derivative was hydrogenated and hydrolyzed to obtain 1-aminomethyltetrahydroquinoline, which was successively acylated with cyclohexanecarbonyl chloride and chloroacetyl chloride, and finally dehydrochlorinated to obtain praziquantel. Isoquinoline can also be used as raw material, through Reissert reaction, cyano group and nitrogen are introduced into 1-position for benzoylation, and then hydrogenated, and the benzoyl group is transferred to the amino group of the side chain, and then chlorine is introduced into the amino group on the ring. Acetyl group, then cyclization, hydrolysis, cyclohexanylformylation to obtain praziquantel [1].
use
Broad-spectrum antiparasitic drug. For the treatment and prevention of schistosomiasis, cysticercosis, paragonimiasis, hydatid disease, fascioliasis, echinococcosis, helminth infection, etc.
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