Praziquantel is an anthelmintic used in humans and animals to treat aphids and trematodes. It is especially effective for schistosomiasis, Chinese schistosomiasis, and Diphyllobothium latum. Praziquantel is a drug on the World Health Organization's list of essential medicines and is one of the most important drugs for basic public health in the world.
Production Method:
After acylation with phenylethylamine as raw material, amination reaction with potassium phthalic acid amide is carried out to introduce an amino group, and cyclized to give 3,4-dihydroisoquinoline under the action of phosphorus oxychloride. The derivative is hydrogenated and hydrolyzed to obtain 1-aminomethyltetrahydroquinoline, which is then acylated with cyclohexanoyl chloride and chloroacetyl chloride, and finally dehydrochlorinated to obtain praziquantel. It is also possible to use isoquinoline as a raw material, and benzoylation by introducing a cyano group and a nitrogen at the 1-position by a Reissert reaction, followed by hydrogenation, while the benzoyl group is transferred to the amino group of the side chain, and chlorine is introduced to the amino group on the ring. Acetyl, then cyclized, hydrolyzed, cyclohexylated to give praziquantel.
Usage:
A broad spectrum anti-parasitic drug. For the treatment and prevention of schistosomiasis, cysticercosis, paragonimiasis, echinococcosis, ginger schistosomiasis, hydatidosis, helminth infection, etc.
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