Lithium borohydride → HCID 46917447, compound

Participants

Reaction Steps

A solution of lithium borohydride (42.3 mg, 1.94 mmol) in THF (3 ml) was added at 0° C. to a solution of methyl 2-(4-fluorophenyl)-2-(2-(1-(4-(trifluoromethoxy)phenylsulfonyl)piperidin-4-ylidene)acetamido)acetate prepared in EXAMPLE 19 (350 mg, 0.647 mmol) in THF (7 ml) and the whole was stirred at room temperature for 18 hours. The reaction mixture was quenched with H2O and the resulting precipitation was collected and washed with H2O and n-hexane to give N-(1-(4-fluorophenyl)-2-hydroxyethyl)-2-(1-(4-(trifluoromethoxy)phenylsulfonyl)piperidin-4-ylidene)acetamide (298 mg, 92%) as a white solid: LCMS: 503 {M+1}+. 1H NMR (DMSO-d6)□ δ: 2.27 (m, 2H), 2.98-3.06 (m, 6H), 3.51 (m, 2H), 4.84 (m, 2H), 5.78 (s, 1H), 7.10 (m, 2H), 7.29 (m, 2H), 7.61 (d, 2H), 7.89 (d, 2H), 8.29 (d, 1H).

Provenance & Evidence