Veterinary medicine Raw Materials Praziquantel Powder

CAS:55268-74-1

MF: C19H24N2O2

MW: 312.41

EINECS:259-559-6

Specification​: 99% min Praziquantel Powder

Sample: Praziquantel Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance: powder or crystals

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Praziquantel Usage and Synthesis.

Praziquantel has a significant killing effect on adult schistosomes.

Its insecticidal mechanism, from the molecular level, is that praziquantel rapidly disrupts the Ca2+ balance in the body of the worm, on the one hand, leading to excitation of the worm's activity, muscle contracture, so that the parasite in the portal system of the schistosoma can not be adsorbed on the blood vessel wall and blood flow into the liver (liver shift), and then be damaged; on the other hand, it leads to the damage of schistosoma's syncytiotrophoblastic cortex, in addition to making the worm's absorption, excretion and secretion functions affected, resulting in the disorders of glucose metabolism, enzyme system and so on. In addition to affecting the absorption, excretion and secretion functions of the parasite, resulting in disorders of glucose metabolism and enzyme systems, the exposure of antigenic determinants on the body surface of the parasite is recognised by the host's immune system, attracting a large number of inflammatory cells, such as neutrophils, eosinophils, and macrophages, to gather around the parasite and exert an attack.

Uses and functions of Praziquantel.

Praziquantel is a broad-spectrum antiparasitic drug, effective anthelmintic against Schistosoma japonicum, Schistosoma mansoni and Schistosoma aegypti, Schistosoma oryzae, Schistosoma pulmonarum, Schistosoma gingersnake, cestodes and cysticerci. Especially, it has strong killing effect on tapeworms, and it is the best one among the current schistosomiasis drugs.

Pharmacological Effects of Praziquantel.

Praziquantel is a commonly used drug for the treatment of schistosomiasis, with 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 pass through the blood and brain barrier of rats, and can enter the bile of dogs, which can prompt the inward flow of Ca2+ outside the membrane of schistosome myocytes, cause muscle contracture, and lose the ability to suction the parasitic site.

At the same time cause sugar metabolism and energy metabolism disorders, "accompanying immune" state is destroyed, and then through the host immune system, and finally eliminate the worm, on the schistosoma, tapeworm, schistosoma, cysticercus and immature worms (caecilians, trichinae) are very good efficacy of killing.

Production Method of  Bulk Praziquantel Powder.

Phenylethylamine as raw material, after acylation with chloroacetyl chloride, then amination reaction with potassium benzenedicarboxamide to introduce the amino group, cyclization under the action of phosphorus trichloride to obtain 3,4-dihydroisoquinoline derivatives, hydrogenation and hydrolysis to obtain 1-aminomethyltetrahydroquinoline, successively acylated with cyclohexanecarbonyl chloride and chloroacetyl chloride, and finally dehydrogenated to obtain the praziquantel by cyclization.

It can also be isoquinoline as raw material, through the Reissert reaction, the introduction of cyano and nitrogen benzoylation in the l position, and then hydrogenation, at the same time, benzoyl transfer to the amino group of the side chain, and then the introduction of chloroacetyl chloride on the amino group on the ring, and then cyclization, hydrolysis, and cyclohexanecarbonyl chloride to get the praziquantel.