- Novel preparation method of albendazole
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The invention provides a novel preparation method of albendazole. According to the invention, a novel synthetic route of albendazole is provided, wherein 2-nitro-5-chloroaniline is used as a startingmaterial and is subjected to reactions of substitution, condensation, reduction and cyclization to obtain high-purity albendazole. The method is characterized in that: the 2-nitro-5-chloroaniline is subjected to substituted reaction, and is subjected to condensation reaction with halogenated n-propane to obtain 2-nitro-5-albendazole aniline, which avoids the use of propanethiol with a high price and a stimulating odor. The use of a high-risk hydrogenation reduction process is avoided, a vulcanization alkali reduction process which is cheap and easily available in raw materials is used, a set of non-toxic treatment schemes for reducing layered waste water are provided, and meanwhile, secondary sodium thiosulfate can be obtained and the waste is turned into wealth. According to the method, the yield is high, the safety risk is low, the industrial production is facilitated, the content of the prepared albendazole is high, the content of single impurities is small, and the latest standardssuch as the US Pharmacopeia and the European Pharmacopoeia are met.
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Paragraph 0059-0061
(2019/01/05)
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- Synthesis and antiparasitic activity of Albendazole and Mebendazole analogues
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Albendazole (Abz) and Mebendazole (Mbz) analogues have been synthesized and in vitro tested against the protozoa Giardia lamblia, Trichomonas vaginalis and the helminths Trichinella spiralis and Caenorhabditis elegans. Results indicate that compounds 4a, 4b (Abz analogues), 12b and 20 (Mbz analogues) are as active as antiprotozoal agents as Metronidazole against G. lamblia. Compound 9 was 58 times more active than Abz against T. vaginalis. Compounds 8 and 4a also shown high activity against this protozoan. Compounds 4b and 5a were as active as Abz. None of the Mbz analogues showed activity against T. vaginalis. The anthelmintic activity presented by these compounds was poor.
- Navarrete-Vazquez, Gabriel,Yepez, Lilian,Hernandez-Campos, Alicia,Tapia, Amparo,Hernandez-Luis, Francisco,Cedillo, Roberto,Gonzalez, Jose,Martinez-Fernandez, Antonio,Martinez-Grueiro, Mercedes,Castillo, Rafael
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p. 4615 - 4622
(2007/10/03)
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- Preparation of N-methoxycarbonyl-N'-[2-nitro-4(5)-propyl-thiophenyl]thiourea as prodrugs of albendazole
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N-methoxycarbonyl-N'-(2-nitro-4-propylthiophenyl)thiourea and N-methoxycarbonyl-N'-(2-nitro-5-propylthiophenyl)thiourea, prodrugs of albendazole, have been synthesized. The biotransformation in rats, after oral administration of these prodrugs to albendazole and albendazole sulphoxide, is described.
- Hernandez-Luis, Francisco,Castillo, Rafael,Yepez-Mulia, Lilian,Cedillo-Rivera, Roberto,Martinez-Vazquez, Gabriel,Morales-Hurtado, Raul,Jung, Helgi,Sanchez, Monica,Hernandez-Campos, Alicia,Viveros, Noemi,Munoz, Onofre
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p. 2231 - 2236
(2007/10/03)
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