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

HRID 343

反応式

HRID 343 の反応式
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

参加物

7

反応条件

温度
50 °C

実験手順

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 %)

出典と根拠

ORDレコード
ord-8809d217cb404d41bb5809dd5f95b269
出典データセット
750 AstraZeneca ELN dataset
元リンク
出典を表示

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