Methylamine → HCID 86694423, compound

Participants

Reaction Conditions

Reaction Steps

Under stirring at 0° C. 2-bromopropanoyl bromide (44 μl, 0.42 mmol) is added dropwise to a mixture of 6-(2-phenylethynyl)-5-pyrimidin-5-yl-4-(trifluoromethyl)pyridin-2-amine C3d (95 mg, 0.28 mmol), triethylamine (59 μl, 0.42 mmol), DMAP (0.3 mg, 3 μmol) and dioxane (1.4 ml). The mixture is warmed to RT and stirred for 1 h. Methylamine (solution in THF 2 mol/l, 1.4 ml, 2.8 mmol) is added and stirring continued for 6 h. The mixture is concentrated in vacuo and the product purified by RP HPLC. Yield: 45 mg (38%). HPLC-MS: M+H=426; tR=1.27 min (*Method—1).

Provenance & Evidence