856058-00-9Relevant academic research and scientific papers
Synthesis of pyrazolones and pyrazoles via Pd-catalyzed aerobic oxidative dehydrogenation
Zhu, Ye-Fu,Wei, Bo-Le,Wei, Jiao-Jiao,Wang, Wen-Qiong,Song, Wei-Bin,Xuan, Li-Jiang
supporting information, p. 1202 - 1205 (2019/03/29)
A palladium-catalyzed oxidative dehydrogenation reaction in the presence of AMS and base to synthesize pyrazolones and pyrazoles was identified. This method can be utilized to a wide range of substrates, operates under mild react conditions and can give high yields. We believe it could be used as an alternative protocol for the classical dehydrogenation reactions.
1-(3′-[125I]iodophenyl)-3-methy-2-pyrazolin-5-one: Preparation, solution stability, and biodistribution in normal mice
Sano, Yuuhei,Motomura, Tomokazu,Yamamoto, Fumihiko,Fukuda, Miki,Mukai, Takahiro,Maeda, Minoru
experimental part, p. 1020 - 1025 (2010/11/04)
3-Methyl-1-phenyl-2-pyrazolin-5-one (edaravone, 1), known as a potent free radical scavenger, has been developed as a medical drug for the treatment of acute cerebral infarction. With the aim of developing radiotracers for imaging free radicals in vivo, 1-(3′-[125I]iodophenyl)-3-methy-2- pyrazolin-5-one (125I-2) was synthesized by two methods, via isotopic exchange and interhalogen exchange under solvent-free conditions, in which iodo- and bromo-derivatives were used as labeling precursors, respectively. After HPLC purification, 125I-2 was obtained in modest isolated radiochemical yields (ca. 20%) with high radiochemical purities by both methods. The former gave specific activities of 0.2-0.6 kBq/μmol, whereas the latter approach achieved specific activities of more than 0.14 GBq/μmol. On attempting to prepare an injectable formulation for 125I-2 with high specific activity, its radiochemical purities dropped to about 60-70%. Unlabeled analog 2 was found to have lipophilic and antioxidant properties similar to edaravone. Intravenous injection of 125I-2 with low specific radioactivity into normal mice showed signs of distribution profiles similar to reported results for 14C-labeled edaravone in normal rats.
