Methyl iodide → 1-(4-Benzylpiperazin-1-yl)-3-methyltetrahydropyrimidin-2(1H)-one

Lithium bis(trimethylsilyl)amide (1M THF solution; 1.5 mL) was added to a solution of 1-(4-benzylpiperazin-1-yl)tetrahydropyrimidin-2(1H)-one (0.27 g) obtained in Example 25a) in THF (10 mL) at 0° C., and the mixture was stirred at room temperature for one hour. Methyl iodide (0.09 mL) was added thereto, and the mixture was stirred at room temperature for 15 hours. The reaction mixture was concentrated under reduced pressure, and the residue was diluted with an aqueous sodium bicarbonate solution, and extracted with dichloromethane. The extract was dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure to obtain the title compound (0.30 g, quantitative) as a brown oil.

1. stirringthe mixture was stirred at room temperature for 15 hours
2. concentrationThe reaction mixture was concentrated under reduced pressure
3. additionthe residue was diluted with an aqueous sodium bicarbonate solution
4. extractionextracted with dichloromethane
5. dry with materialThe extract was dried over anhydrous sodium sulfate
6. distillationthe solvent was distilled off under reduced pressure

ORD record

ord-576aec26067c4544b215ef8f9df8c15b

Source dataset

uspto-grants-2010_06

DOI

10.6084/m9.figshare.5104873.v1

Patent number

US07745623B2