Methylamine → HCID 23627796, compound

Participants

Reaction Steps

A solution of [(S)-2-Benzyl-4-(3-cyclopentyloxy-4-methoxy-phenyl)-piperazin-1-yl]-acetic acid (Example 59) (21.2 mg, 0.05 mmol) in CH2Cl2 (0.5 mL) at 0° C. was treated with DMAP (˜1 mg) and DCC (11.3 mg, 0.055 mmol) followed 5 min later by a 2 M THF solution of methylamine (30 μL, 0.06 mmol). The reaction mixture was stirred for 16 h, evaporated, and purified by silica gel flash chromatography with 50% EtOAc/hexane, then 100% EtOAc, then 5% MeOH/EtOAc as eluant to afford product as an oil (6.4 mg, 29%). LC/MS 5.09 min, [M+1]+ 438.

Provenance & Evidence