1-Bromo-4-fluorobenzene → 1-Benzyl-4-(4-fluorophenyl)piperazine

HRID 343

Reaktionsgleichung

Reaktionsgleichung von HRID 343
Fc1ccc(Br)cc1.c1ccc(CN2CCNCC2)cc1>CC(=O)O.CC(=O)O.CC(C)(C)[O-].CC1(C)c2cccc(P(c3ccccc3)c3ccccc3)c2Oc2c(P(c3ccccc3)c3ccccc3)cccc21.Cc1ccccc1.[Na+].[Pd]>Fc1ccc(N2CCN(Cc3ccccc3)CC2)cc1

Komponenten

7

Reaktionsbedingungen

Temperatur
50 °C

Versuchsvorschrift

diacetoxypalladium (12.74 mg, 0.06 mmol) and (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (32.8 mg, 0.06 mmol) were suspended in toluene (0.5 mL) under N2. Heated to 50C for 30 min (microwave). sodium 2-methylpropan-2-olate (109 mg, 1.13 mmol) was suspended in toluene (0.500 mL) under N2. 1-benzylpiperazine (0.099 mL, 0.57 mmol) and 1-bromo-4-fluorobenzene (0.093 mL, 0.85 mmol) were added, followed by the catalyst solution. Heated to 100C for 2h in the microwave (high abs), then rt over night. The product was purified on silica (0-25% EtOAc/heptane) Yield: 1-benzyl-4-(4-fluorophenyl)piperazine (115 mg, 75.0 %)

Quellen und Nachweise

ORD-Eintrag
ord-8809d217cb404d41bb5809dd5f95b269
Quelldatensatz
750 AstraZeneca ELN dataset
Originallink
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