Praziquantel CAS 55268-74-1 Raw Materials Powder

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Praziquantel Powder Usage and Synthesis.

Praziquantel Powder (praziquantel) is a broad-spectrum anthelmintic synthetic drug discovered in the 1970s, which is highly effective against It is a colorless crystalline powder, odorless and slightly bitter, stable under normal conditions. 

Praziquantel CAS 55268-74-1 is a broad-spectrum anthelmintic, effective against Schistosoma japonicum, Schistosoma mansoni and Schistosoma egypti It is a broad-spectrum anthelmintic, effective against Schistosoma japonicum, Schistosoma mansoni and Schistosoma egypti, Schistosoma mansoni, Schistosoma haematobium, Schistosoma lungworm, Schistosoma gingerbread, cestode and cysticercus. 

Praziquantel Raw Materials has a significant killing effect on adult schistosomes.

Application/Function of Praziquantel Powder.

Praziquantel is a commonly used drug for the treatment of schistosomiasis. It has minimal toxicity to animals and is rapidly absorbed in the digestive tract after oral administration. Peak blood time: 5 minutes in mice, l5-30 minutes in rats, 30-120 minutes in dogs, and about 2h in sheep.

After absorption, the drug is widely distributed in all tissues and organs, and can even cross the blood-brain barrier in rats, and can enter the bile of dogs, which can induce the inward flow of Ca2+ outside the myocyte membrane of schistosomes, causing muscle contraction and loss of the ability to suck on the parasitic site. At the same time, it causes disorders of glucose metabolism and energy metabolism, and the state of "concomitant immunity" is destroyed, and then the host immune system is finally destroyed.

Histochemical observations from in vivo and in vitro tests showed that schistosomal glycogen was significantly reduced, ribonucleic acid and alkaline phosphatase were decreased, and the activity of alkaline protein reaction or acid phosphatase was increased after the action of the drug.

Praziquantel is a broad-spectrum antihelmintic, effective against Schistosoma japonicum, Schistosoma mansoni and Schistosoma egypti, Schistosoma mansoni, Schistosoma haematobium, Schistosoma lungeri, Schistosoma gingerbread, Cestodes and Cysticerci. It is the most effective anthelmintic for schistosomes, especially for cestodes, and has the best results among schistosomiasis drugs.

Production Method of Praziquantel Powder

Praziquantel has a significant effect on killing adult schistosomes. The mechanism of killing, from the molecular level, is that praziquantel rapidly disrupts the Ca2+ balance in the body of schistosomes, which leads to excitement and muscle contraction,

so that schistosomes parasitized in the portal system cannot attach to the blood vessel wall and are carried to the liver by the blood flow (hepatic shift), and are then damaged; secondly, it causes damage to the syncytial cortex of schistosomes, which not only affects the absorption, excretion and secretion functions of schistosomes, but also leads to disorders of glucose metabolism and enzyme system.

In addition to the disruption of glucose metabolism and enzymatic systems, the antigenic determinants on the surface of the worm are exposed and recognized by the host's immune system, attracting a large number of inflammatory cells such as neutrophils, eosinophils and macrophages to gather around the worm and attack it.

Production Method of Praziquantel Powder

• 1. Phenylethylamine is used as raw material, and then amidated with chloroacetyl chloride, followed by amination with potassium benzodicarbonate to introduce the amino group, and then cyclized with trichloroxaphos to obtain 3,4-dihydroisoquinoline derivatives, which are hydrogenated and hydrolyzed to obtain 1-aminomethyltetrahydroquinoline, successively acylated with cyclohexanecarbonyl chloride and chloroacetyl chloride, and finally cyclized with dechlorinated hydrogen to obtain praziquantel.

• 2. Isoquinoline is used as raw material, by Reissert reaction, introducing cyano and benzoylation on nitrogen at the l-position, then hydrogenation, while benzoyl is transferred to the amino group of the side chain, and then introducing chloroacetyl on the amino group of the ring, then cyclization, hydrolysis and cyclohexanecarbonylation to get praziquantel.

• There are various synthetic routes in industrial production: isoquinoline route, piperazine route and phenylethylamine route, among which the quinoline route is better. Isoquinoline is added with benzoyl chloride and potassium cyanide, catalyzed hydrogenation and rearrangement to obtain 1-benzoylaminomethyl-1,2,3,4-tetrahydroisoquinoline, then chloroacetylation, cyclization, pressurized hydrolysis and cyclohexanecarbonylation to obtain praziquantel.

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