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

HRID 239笔记

反应方程式

HRID 239 反应方程式
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

参与物

7

反应条件

温度
80 °C

实验过程

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.

来源与证据

ORD记录
ord-bddc6734b7ce4143a8ed8f8385933b6e
来源数据集
750 AstraZeneca ELN dataset
原始链接
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反应笔记

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