4-Aminomethyltetrahydropyran → 3-Bromo-4-methoxy-N-[(oxan-4-yl)methyl]aniline

HRID 472

반응식

HRID 472 반응식
COc1ccc(I)cc1Br.NCC1CCOCC1>C1COCCO1.CC(=O)O.CC(=O)O.CC(C)(C)[O-].[Na+].[Pd].c1ccc(P(c2ccccc2)c2ccc3ccccc3c2-c2c(P(c3ccccc3)c3ccccc3)ccc3ccccc23)cc1>COc1ccc(NCC2CCOCC2)cc1Br

참가 물질

7

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온도
80 °C

실험 절차

Palladium (II) acetate (0.075 g, 0.34 mmol) and racemic-2,2'-Bis(diphenylphosphino)-1,1'-binaphthyl (0.223 g, 0.36 mmol) were suspended in dioxane (5mL). The mixture was evacuated and purged with nitrogen, and warmed to 50°C. In a separate vessel, 2-bromo-4-iodo-1-methoxybenzene (1.4 g, 4.47 mmol), (tetrahydro-2H-pyran-4-yl)methanamine (0.547 mL, 4.47 mmol) and sodium-t- butoxide (0.645 g, 6.71 mmol) were suspended in dioxane (5ML). The resulting mixture was evacuated, purged with nitrogen and warmed to 50°C. After ~30 mins, the catalyst mixture was transferred to the reaction vessel. The reaction was evacuated and purged with nitrogen and heated at 80°C overnight. Very little product and mainly SM so reaction abandoned.

출처 및 근거

ORD 기록
ord-6117c2ee846f49c3a77484ecf172e880
출처 데이터셋
750 AstraZeneca ELN dataset
원본 링크
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