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- W1608524596 abstract "[13CD3]-TAK-459 (1A), an HSP90 inhibitor, was synthesized from [13CD3]-sodium methoxide in three steps in an overall yield of 29%. The key intermediate [13CD3]-2-methoxy-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine was synthesized in two steps from 2,6-dibromopyridine and stable isotope-labeled sodium methoxide. [14C]-TAK-459 (1B) was synthesized from [14C(U)]-guanidine hydrochloride in five steps in an overall radiochemical yield of 5.4%. The key intermediate, [14C]-(R)-2-amino-7-(2-bromo-4-fluorophenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one, was prepared by microwave-assisted condensation." @default.
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- W1608524596 date "2014-07-01" @default.
- W1608524596 modified "2023-09-24" @default.
- W1608524596 title "Synthesis of isotope-labeled HSP90 inhibitor: [13CD3] and [14C]-TAK-459" @default.
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- W1608524596 doi "https://doi.org/10.1002/jlcr.3217" @default.
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