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温度

0 °C

(3S)—N,N-Dimethyl-5-oxo-4-(phenylmethyl)-3 morpholinecarboxamide (390 mg, 1.5 mmol) was dissolved in THF (20 mL) and the solution was cooled to 0° C. LiAlH4 (225 mg, 5.9 mmol) was added and the resulting mixture was refluxed overnight. Upon cooling to 0° C., water (1.4 mL) was added followed by 15% (w/w) NaOH (aq) (1.4 mL) and finally another portion of water (4.2 mL). Stirring for 30 min followed by filtration and concentration in vacuo yielded a crude mixture which was purified by RP-HPLC to provide dimethyl{[(3R)-4-(phenylmethyl)-3-morpholinyl]methyl}amine (510 mg, 41%). LCMS: (M+H)+: 235.2.

1. temperaturethe resulting mixture was refluxed overnight
2. temperatureUpon cooling to 0° C.
3. filtrationfollowed by filtration and concentration in vacuo
4. customyielded a crude mixture which
5. customwas purified by RP-HPLC