Morpholine → Ethyl 5-morpholin-4-ylpyridine-3-carboxylate

反応式

C1COCCN1.CCOC(=O)c1cncc(Br)c1>C1COCCO1.CC(C)(C)[O-].CN(C)c1ccccc1-c1ccccc1P(C1CCCCC1)C1CCCCC1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.[Na+].[Pd].[Pd]>CCOC(=O)c1cncc(N2CCOCC2)c1

参加物

反応条件

温度: 80 °C

実験手順

ethyl 5-bromonicotinate (200 mg, 0.87 mmol), morpholine (0.083 mL, 0.96 mmol), sodium 2-methylpropan-2-olate (167 mg, 1.74 mmol) and 2'-(dicyclohexylphosphino)-N,N-dimethylbiphenyl-2-amine (17.11 mg, 0.04 mmol) were suspended in dioxane (5 mL). The reaction flask was purged with nitrogen and TRIS(DIBENZYLIDENEACETONE)DIPALLADIUM(0) (19.90 mg, 0.02 mmol) was added. The reaction was stirred at 80 °C for 90 minutes. LCMS analysis appeared to indicate addition of 2 morpholine rings and the reaction was abandoned.