13369-83-0Relevant articles and documents
Tritiated metronidazole and preparation method thereof
-
Paragraph 0013; 0033; 0034, (2017/08/28)
The invention belongs to the field of radioactive isotope labeling preparation, and particularly relates to tritiated metronidazole and a preparation method thereof. The preparation method includes: using 2-methyl-5-nitroimidazole as a raw material to react with N-iodosuccinimide to obtain 4-iodine-2-methyl-5nitroimidazole; under catalysis of palladium carbon, enabling 4-iodine-2-methyl-5nitroimidazole and tritium gas to be in tritium-halogen exchange to generate 4-3H-2-methyl-5-nitroimidazole; enabling 4-3H-2-methyl-5-nitroimidazole to react with ethylene oxide to obtain 4-3H-metronidazole. A synthetic product is purified through a prepared liquid phase to obtain4-3H-metronidazole with high specific activity (22.08Ci/g), high radiochemical purity (greater than or equal to 98%) and high chemical purity (greater than or equal to 98%). The tritiated metronidazole can be used as a radioactive tracer in studying absorption, distribution, metabolism and residue elimination of metronidazole in animal bodies.
Electrophilic iodination of 4-nitroimidazoles - A new high yielding method for the synthesis of 4-nitro-5-iodoimidazoles
Rao,Rao,Singh
, p. 353 - 366 (2007/10/02)
Electrophilic iodination of 4-nitroimidazoles employing the system KI- HNO3-AcOH provided a new route for the synthesis of 4-nitro-5-iodoimidazoles in high yields. With 2-unsubstituted-4-nitroimidazoles, 2,5-diiodo-4- nitroimidazoles were obtained.