2-Bromo-4-nitroanisole → 5-chloro-N-(2-methoxy-5-nitrophenyl)-4-pyrazolo[1,5-a]pyridin-3-ylpyrimidin-2-amine

HRID 420

反応式

HRID 420 の反応式
COc1ccc([N+](=O)[O-])cc1Br.Nc1ncc(Cl)c(-c2cnn3ccccc23)n1>C1COCCO1.CC1(C)c2cccc(P(c3ccccc3)c3ccccc3)c2Oc2c(P(c3ccccc3)c3ccccc3)cccc21.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]>COc1ccc([N+](=O)[O-])cc1Nc1ncc(Cl)c(-c2cnn3ccccc23)n1

参加物

7

反応条件

温度
150 °C

実験手順

_Crude SM used_ 2-bromo-1-methoxy-4-nitrobenzene (0.029 g, 0.13 mmol), 5-chloro-4-(pyrazolo[1,5-a]pyridin-3-yl)pyrimidin-2-amine (0.031 g, 0.125 mmol) and cesium carbonate (0.057 g, 0.18 mmol) were suspended in dry dioxane (2 mL) the mixture degassed with nitrogen for 10 minutes. TRIS(DIBENZYLIDENEACETONE)DIPALLADIUM(0) (0.034 g, 0.04 mmol) and (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (0.029 g, 0.05 mmol) were added and the mixture was sealed into a microwave tube. The reaction was heated to 150 °C for 2 hours in the microwave reactor and cooled to RT. Possibly product - not very much. The reaction was heated to 150 °C for 10 hours in the microwave reactor and cooled to RT. Product now c4%, both starting materials still present. Not continued.

出典と根拠

ORDレコード
ord-d45c4d4f76fd453681edb48cc851d97a
出典データセット
750 AstraZeneca ELN dataset
元リンク
出典を表示

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