一甲胺 → 5-三氟甲基吡啶-3-甲胺

HRID 181

反应方程式

HRID 181 反应方程式
CN.FC(F)(F)c1cncc(Br)c1>C1COCCO1.CC1(C)c2cccc(P(c3ccccc3)c3ccccc3)c2Oc2c(P(c3ccccc3)c3ccccc3)cccc21.ClC(Cl)Cl.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C([O-])[O-].[Cs+].[Cs+].[Pd].[Pd]>CNc1cncc(C(F)(F)F)c1

参与物

7

反应条件

温度
130 °C

实验过程

3-bromo-5-(trifluoromethyl)pyridine (100 mg, 0.44 mmol), methylamine 2 M in THF (0.442 mL, 0.88 mmol), and cesium carbonate (202 mg, 0.62 mmol) were suspended in dioxane (3 mL) . The reaction was purged with nitrogen for 30 minutes then 9,9-Dimethyl-4,5-bis(diphenylphosphino)xanthene (7.68 mg, 0.01 mmol) and TRIS(DIBENZYLIDENEACETONE)DIPALLADIUM(0)-CHLOROFORM ADDUCT (9.16 mg, 8.85 µmol) were added. The reaction was heated at 130 c for 30mins. No REACTION ABANDONED

来源与证据

ORD记录
ord-6eff375bd801443f9df865a891f3e022
来源数据集
750 AstraZeneca ELN dataset
原始链接
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