Electric Literature of 121-66-4, An article , which mentions 121-66-4, molecular formula is C3H3N3O2S. The compound – 5-Nitrothiazol-2-amine played an important role in people’s production and life.
The highly selective glycogen synthase kinase-3 (GSK-3) inhibitor N-(4-methoxybenzyl)-N?-(5-nitro-1,3-thiazol-2-yl)urea (AR-A014418) was radiolabeled with carbon-11 (11C; half-life = 20.4 min) at the urea moiety via [11C]CO2 fixation. Reaction of [ 11C]CO2 with 4-methoxybenzylamine in the presence of a CO2 fixating base was followed by dehydration with POCl3 and addition of 2-amino-5-nitrothiazole to prepare [11C-carbonyl] AR-A014418. This reaction resulted in an 8% uncorrected radiochemical yield, based on [11C]CO2, with high specific activity (4 Ci/mumol) within 30 min. An in vitro GSK-3beta enzyme activity assay revealed that AR-A014418 (Ki = 770 nM) is not as potent as previously claimed. The [11C]CO2 fixation methodology described herein should prove generally applicable to preparing 1-aryl-3-benzyl-[ 11C-carbonyl] ureas as radiotracers for positron emission tomography.
The highly selective glycogen synthase kinase-3 (GSK-3) inhibitor N-(4-methoxybenzyl)-N?-(5-nitro-1,3-thiazol-2-yl)urea (AR-A014418) was radiolabeled with carbon-11 (11C; half-life = 20.4 min) at the urea moiety via [11C]CO2 fixation. Reaction of [ 11C]CO2 with 4-methoxybenzylamine in the presence of a CO2 fixating base was followed by dehydration with POCl3 and addition of 2-amino-5-nitrothiazole to prepare [11C-carbonyl] AR-A014418. This reaction resulted in an 8% uncorrected radiochemical yield, based on [11C]CO2, with high specific activity (4 Ci/mumol) within 30 min. An in vitro GSK-3beta enzyme activity assay revealed that AR-A014418 (Ki = 770 nM) is not as potent as previously claimed. The [11C]CO2 fixation methodology described herein should prove generally applicable to preparing 1-aryl-3-benzyl-[ 11C-carbonyl] ureas as radiotracers for positron emission tomography.
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Reference£º
Thiazole | C3H9427NS – PubChem,
Thiazole | chemical compound | Britannica