Piperazine, 2-pyridylethyl- → Ethyl 7-(4-(2-(pyridin-2-yl)ethyl)piperazin-1-yl)benzofuran-2-carboxylate

HRID 99

반응식

HRID 99 반응식
CCOC(=O)c1cc2cccc(Br)c2o1.c1ccc(CCN2CCNCC2)nc1>C1COCCO1.CC(C)c1cc(C(C)C)c(-c2ccccc2P(C2CCCCC2)C2CCCCC2)c(C(C)C)c1.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]>CCOC(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1

참가 물질

7

반응 조건

온도
95 °C

실험 절차

The reaction mixture of ethyl 7-bromobenzofuran-2-carboxylate (2.0 g, 7.43 mmol), 1-(2-(pyridin-2-yl)ethyl)piperazine (1.564 g, 8.18 mmol), Tris(dibenzylideneacetone)dipalladium(0) (0.476 g, 0.52 mmol), 2-Dicyclohexylphosphino-2',4',6'-tri-iso-propyl-1,1'-biphenyl (0.496 g, 1.04 mmol) and Cesium carbonate (3.63 g, 11.15 mmol) in dioxane (30 mL) (degassed with argon for 10 min) was heated at 95 °C under argon for 5 h. After cooling, the reaction mixture was filtered and concentrated. The product was purified twice by isco, the first using DCM:MeOH (0-5%) and the second time using DCM:MeOH (0-3%).

출처 및 근거

ORD 기록
ord-d491779c6ebc428d97eb810ae5444bf6
출처 데이터셋
750 AstraZeneca ELN dataset
원본 링크
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