1,6-Dioxaspiro[2.5]octane → 4-{[(2R,5S)-4-benzyl-2,5-dimethylpiperazin-1-yl]methyl}tetrahydro-2H-pyran-4-ol

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To a microwave vial was added 1,6-dioxaspiro[2.5]octane (259 mg, 2.3 mmol), (2S,5R)-1-benzyl-2,5-dimethylpiperazine (464 mg, 2.3 mmol) and 5 mL of MeOH. The vial was heated to 150° C. for 2 h in the microwave. The crude reaction was concentrated to provide intermediate H1(ii) (723 mg, 100%) 1H NMR (300 MHz, CHLOROFORM-d) δ ppm 0.92 (d, J=6.22 Hz, 3H), 1.13 (d, J=5.84 Hz, 3H), 1.35-1.45 (m, 1H), 1.46-1.68 (m, 4H), 1.83 (dd, J=11.30, 9.80 Hz, 1H), 2.12 (d, J=13.94 Hz, 1H), 2.36-2.53 (m, 3H), 2.60-2.69 (m, 2H), 2.85 (d, J=9.04 Hz, 1H), 3.08 (d, J=13.38 Hz, 1H), 3.71-3.82 (m, 4H), 4.04 (d, J=13.38 Hz, 1H), 7.10-7.47 (m, 5H). Mass Spectrum: Calcd for C19H30N2O2 (M+H): 318. Found: 318.

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