반응 #813

ord-dcac8bcfa5124a8baee8e28e5e992678

반응 방정식

COc1ccc(Br)cc1OC
COc1ccc(Br)cc1OC
CC(C)[C@@H]1CNCCN1C(=O)OC(C)(C)C
CC(C)[C@@H]1CNCCN1C(
COc1ccc(N2CCN(C(=O)OC(C)(C)C)[C@H](C(C)C)C2)cc1OC
COc1ccc(N2CCN(C(=O)O
수율 90.5%

용매

반응 조건

온도
150°CELSIUS

실험 절차

22-Apr-09 09:56:23 +0100 4-bromo-1,2-dimethoxybenzene (0.068 mL, 0.46 mmol), (R)-tert-butyl 2-isopropylpiperazine-1-carboxylate (126 mg, 0.55 mmol) and BIS(TRI-T- BUTYLPHOSPHINE)PALLADIUM(0) (23.54 mg, 0.05 mmol) and potassium 2-methylpropan-2-olate (76 mg, 0.64 mmol) were suspended in THF (5 mL) and sealed into a microwave tube. The reaction was heated to 150 °C for 10 minutes in the microwave reactor and cooled to RT. LC-MS shows no starting material. The reaction mixture was filtered and the crude product was purified by flash silica chromatography, elution gradient 0 to 20% EtOAc in isohexane. Pure fractions were evaporated to dryness to afford (R)-tert-butyl 4-(3,4-dimethoxyphenyl)-2-isopropylpiperazine-1-carboxylate (152 mg, 91 %) as a yellow gum.

출처

750 AstraZeneca ELN dataset