p-Bromoacetophenone → Tert-butyl 4-(4-acetylphenyl)piperazine-1-carboxylate

HRID 557

Reaktionsgleichung

Reaktionsgleichung von HRID 557
CC(=O)c1ccc(Br)cc1.CC(C)(C)OC(=O)N1CCNCC1>CC(=O)O.CC(=O)O.Cc1ccccc1.O=C([O-])[O-].[Cs+].[Cs+].[Pd].c1ccc(P(c2ccccc2)c2ccc3ccccc3c2-c2c(P(c3ccccc3)c3ccccc3)ccc3ccccc23)cc1>CC(=O)c1ccc(N2CCN(C(=O)OC(C)(C)C)CC2)cc1

Komponenten

7

Reaktionsbedingungen

Temperatur
120 °C

Versuchsvorschrift

In a CEM MW vial, p-Bromoacetophenone (729 ml, 6.03 mmol),tert-Butyl 1-piperazinecarboxylate (1.684 g, 9.04 mmol),racemic-2,2'-Bis(diphenylphosphino)-1,1'-binaphthyl (0.375 g, 0.60 mmol),Palladium (II) acetate (0.135 g, 0.60 mmol),Cesium carbonate (3.93 g, 12.06 mmol) was taken in toluene (10 ml).The RM was subjected to MW power of 300W,temp 120°C for 45 minutes. The LCMS was checked showed the formation of required mass. Work-up: The RM was passed through hyflow bed and filtrate was evaporated and chrmatographed using Ethyl acetate hexane to obtain tert-butyl 4-(4-acetylphenyl)piperazine-1-carboxylate (0.963 g, 52.5 %).

Quellen und Nachweise

ORD-Eintrag
ord-c7d1825ed35e4dffbc57a0b9b8fa9354
Quelldatensatz
750 AstraZeneca ELN dataset
Originallink
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