1394389-41-3Relevant academic research and scientific papers
Synthesis of [11C]Am80 via novel Pd(0)-mediated rapid [ 11C]carbonylation using arylboronate and [11C]Carbon Monoxide
Takashima-Hirano, Misato,Ishii, Hideki,Suzuki, Masaaki
, p. 804 - 807,4 (2012)
11C-labeled methylbenzoates [11C]4a-d were synthesized using Pd(0)-mediated rapid cross-coupling reactions employing [ 11C]carbon monoxide and arylboronic acid neopentyl glycol esters 3a-d under atmospheric pressure in methanol-dimethylformamide (MeOH-DMF), in radiochemical yields of 12 ± 5-26 ± 13% (decay-corrected based on [11C]O). The reaction conditions were highly favorable for the synthesis of [11C]Am80 ([11C]2) and [11C]methyl 4-((5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)carbamoyl)benzoate ([11C]2-Me) using 4-(5,5-dimethyl-1,3,2-dioxaborinan-2-yl)-N-(5,5,8, 8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)benzamide (5), both of which produced a decay-corrected radiochemical yield (RCY) of 26 ± 13%, with >99% radiochemical purity and an average specific radioactivity of 44 GBq/μmol. The yields of [11C]4a, [11C]2-Me, and [ 11C]2 were improved by the use of a 2-fold excess of the solvents and reagents under the same conditions to give respective yields of 66 ± 8, 65 ± 7, and 48 ± 2%.
Synthesis of [11C]Am80 via novel Pd(0)-mediated rapid [ 11C]carbonylation using arylboronate and [11C]Carbon Monoxide
Takashima-Hirano, Misato,Ishii, Hideki,Suzuki, Masaaki
supporting information, p. 804 - 807 (2013/01/15)
11C-labeled methylbenzoates [11C]4a-d were synthesized using Pd(0)-mediated rapid cross-coupling reactions employing [ 11C]carbon monoxide and arylboronic acid neopentyl glycol esters 3a-d under atmospheric pressure in methanol-dimethylformamide (MeOH-DMF), in radiochemical yields of 12 ± 5-26 ± 13% (decay-corrected based on [11C]O). The reaction conditions were highly favorable for the synthesis of [11C]Am80 ([11C]2) and [11C]methyl 4-((5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)carbamoyl)benzoate ([11C]2-Me) using 4-(5,5-dimethyl-1,3,2-dioxaborinan-2-yl)-N-(5,5,8, 8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)benzamide (5), both of which produced a decay-corrected radiochemical yield (RCY) of 26 ± 13%, with >99% radiochemical purity and an average specific radioactivity of 44 GBq/μmol. The yields of [11C]4a, [11C]2-Me, and [ 11C]2 were improved by the use of a 2-fold excess of the solvents and reagents under the same conditions to give respective yields of 66 ± 8, 65 ± 7, and 48 ± 2%.
