1265131-65-4Relevant academic research and scientific papers
The first synthesis of [11C]SB-216763, a new potential PET agent for imaging of glycogen synthase kinase-3 (GSK-3)
Wang, Min,Gao, Mingzhang,Miller, Kathy D.,Sledge, George W.,Hutchins, Gary D.,Zheng, Qi-Huang
experimental part, p. 245 - 249 (2011/02/27)
SB-216763 is a novel, potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor with an IC50 value of 34 nM. [11C]SB- 216763 (3-(2,4-dichlorophenyl)-4-(1-[11C]methyl-1H-indol-3-yl)-1H- pyrrole-2,5-dione), a new potential PET agent for imaging of GSK-3, was first designed and synthesized in 20-30% decay corrected radiochemical yield and 370-555 GBq/μmol specific activity at end of bombardment (EOB). The synthetic strategy was to prepare a carbon-11-labeled maleic anhydride intermediate followed by the conversion to maleimide.
New heterocycles of 2,3-diaryl-substituted maleic hydrazides
Shih, Hsiencheng,Shih, Renshuay J.,Carson, Dennis A.
experimental part, p. 1243 - 1250 (2012/01/04)
2,3-Diaryl-substituted maleic anhydrides were prepared by a modified one-pot synthesis of Perkin condensation using mixed sodium salts of arylglyoxylic acid and arylacetic acid with acetic anhydride in 1,4-dioxane. The treatment of these anhydrides with ammonium bicarbonate, or methanolic hydrazine, offered the corresponding 2,3-diaryl-substituted maleimides and maleic hydrazides (4,5-diaryl-substituted 1,2-dihydropyridazine-3,6-dione), respectively. Evidence obtained from NMR, UV, and mass spectra suggest that 2,3-diaryl-substituted maleic hydrazides do not exhibit monolactim forms. Ring contraction of the diaryl-substituted maleic hydrazide by nitrosation led to the formation of the corresponding maleimide. Interconversion between the corresponding maleic hydrazide and maleimide was observed following equilibrium reaction. Our experiment proposes that the chemistry of 2,3-diaryl-substituted maleic hydrazides rarely involves the function of ethylene moiety and resembles that of succinic hydrazine. Copyright
