tert-Butyl piperazine-1-carboxylate → tert-butyl 4-(1H-indol-7-yl)piperazine-1-carboxylate

온도

100 °C

2-Dicyclohexylphosphino-2',6'-di-i-propoxy-1,1'-biphenyl (75 mg, 0.16 mmol) and palladium (II) acetate (18.08 mg, 0.08 mmol) were dissoved in toluene (2 mL) at ambient temperature. The mixture was degassed and purged with nitrogen and warmed to 50°C for 20 mins. In a separate vessel, were mixed tert-butyl piperazine-1-carboxylate (300 mg, 1.61 mmol), 7-bromo-1H-indole (316 mg, 1.61 mmol) and sodium-t-butoxide (296 mL, 2.42 mmol) in toluene (3 mL). The mixture was degasssed and purged with nitrogen and warmed to 50°C. The catalyst solution was added to the reaction vessel and the resulting mixture was degassed and purged with nitrogen and heated at 100°C for overnight. UPLC analysis showed virtually no reaction (only 7% conversion to product). Reaction abandoned.

ORD 기록

ord-b6527d32ba054a8395bc5ea7808e53a8

출처 데이터셋

750 AstraZeneca ELN dataset

원본 링크

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