1-Methylpiperazine → 1-(4-Chloro-2-methoxyphenyl)-4-methylpiperazine
Reaction equation
CN1CCNCC1.COc1cc(Cl)ccc1I>CC(=O)O.CC(=O)O.CC(C)(C)[O-].Cc1ccccc1.[Na+].[Pd].c1ccc(P(c2ccccc2)c2ccc3ccccc3c2-c2c(P(c3ccccc3)c3ccccc3)ccc3ccccc23)cc1>COc1cc(Cl)ccc1N1CCN(C)CC1Participants
7
Reactant 2
Product 1
Reagents, catalysts & solvents 4
Conditions
- Temperature
- 80 °C
Procedure
1-methylpiperazine (0.021 mL, 0.19 mmol) was added to 4-chloro-1-iodo-2-methoxybenzene (50 mg, 0.19 mmol) and sodium 2-methylpropan-2-olate (35.8 mg, 0.37 mmol) in toluene (0.650 mL) and the solution degassed. rac-2,2'-Bis(diphenylphosphino)-1,1'-binaphthyl (11.60 mg, 0.02 mmol) and Palladium II acetate (4.18 mg, 0.02 mmol) were added to the resulting mixture and the vial stirred at 80 °C for 17 hours. LCMS revelead product peak, but not great. Product not isolated.
Sources & evidence
- ORD record
- ord-a9eb8bf838c248b3ad5908714b48274f
- Source dataset
- 750 AstraZeneca ELN dataset
- Original link
- View source
Reaction notes
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