3-Fluoropropan-1-amine → N-{[(2S)-5-Chloro-7-(methylsulfonyl)-2,3-dihydro-1,4-benzodioxin-2-YL]methyl}-3-fluoropropan-1-amine

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Reaction Steps

3-Fluoropropan-1-amine HCl-salt (0.178 g, 1.52 mmol) was basified on a SCX-3 ion exchange column (TEA/MeOH). [(2R)-5-chloro-7-(methylsulfonyl)-2,3-dihydro-1,4-benzodioxin-2-yl]methyl 4-methylbenzenesulfonate (0.027 g, 0.062 mmol) and 3-fluoropropan-1-amine (0.15 M in MeOH/TEA:4/1, 5 ml) was heated under microwave radiation at 120° C. for 1 h 20 min. MS m/z (rel. intensity, 70 eV) 337 (M+, 0.4), 91 (5), 90 (bp), 85 (3), 70 (17), 63 (3).

Provenance & Evidence