Formaldehyde → HCID 178483376, compound

Participants

Reaction Steps

To a stirred solution of the free base of Example 258 (20 mg) in methanol (1 mL) and acetic acid (0.5 mL) with sodium acetate (100 mg), was added 30 μL of formaldehyde (37% aq. solution), followed by NaCNBH3 (15 mg). The mixture was stirred for 15 min, additional formaldehyde (30 μL) and NaCNBH3 were added and the mixture was stirred for 30 min and diluted with ethyl acetate and quenched with 3 mL of NH4OH solution. The organic layer was separated, washed with 1 N NH4OH solution and brine, dried, and concentrated. The residue was converted to its HCl salt as described in Example 257 (23 mg). MS (M+H)+ 454.

Provenance & Evidence