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HRID 2374946作成日:2026年10月26日

2-(Di-tert-butylphosphino)biphenyl → Tert-butyl 3-({5-methyl-7-[3-(trifluoromethyl)phenyl]imidazo[5,1-f][1,2,4]triazin-2-yl}amino)benzylcarbamate

https://huagongshe.com/reaction/2374946

反応式

関与物質

役割名称HCID仕込み量
反応物2-(Di-tert-butylphosphino)biphenylHCID 2734215—
反応物tert-Butyl 3-iodobenzylcarbamateHCID 11645663—
反応物Sodium t-butoxideHCID 23676156—
反応物2-Amino-5-methyl-7-[3-(trifluoromethyl)phenyl]imidazo[5,1-f][1,2,4]triazinHCID 58712001—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
溶媒1,4-DioxaneHCID 31275—
生成物Tert-butyl 3-({5-methyl-7-[3-(trifluoromethyl)phenyl]imidazo[5,1-f][1,2,4]triazin-2-yl}amino)benzylcarbamateHCID 1122575031.2%

反応手順

In a similar manner as described for Example 41, 5-methyl-7-[3-(trifluoromethyl)phenyl]imidazo[5,1-f][1,2,4]triazin-2-amine (Intermediate 45) (0.025 g, 0.09 mmol), tert-butyl 3-iodobenzylcarbamate (0.028 g, 0.09 mmol), Pd2(dba)3 (0.008 g, 0.01 mmol), 2-(Di-t-butylphosphino)biphenyl (0.008 g, 0.03 mmol), and NaOtBu (0.011 g, 0.11 mmol) in 1,4-dioxane (1 mL) gave tert-butyl 3-({5-methyl-7-[3-(trifluoromethyl)phenyl]imidazo[5,1-f][1,2,4]triazin-2-yl}amino)benzylcarbamate (0.014 g) as a yellow solid. 1H NMR (CDCl3): δ8.82 (s, 1H), 8.80 (s, 1H), 8.66 (d, J=7.3 Hz, 1H), 7.79-7.73 (m, 1H), 7.70-7.60 (m, 2H), 7.42-7.28 (m, 4H), 7.18 (bs, 1H), 7.04 (d, J=7.7 Hz, 1H), 4.32 (bs, 2H), 2.61 (s, 3H), 1.46 (s, 9H). MS m/z 499 (M+1).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07462614B2
出典データセットuspto-grants-2008_12
ORD IDord-e0af4b685ad24a00b3de525f56058896
出典メモuspto-grants-2008_12