Cesium carbonate → 4-(8-((4-(2-methoxypropan-2-yl)piperidin-1-yl)methyl)-9-methyl-2-(2-methyl-1H-benzo[d]imidazol-1-yl)-9H-purin-6-yl)morpholine

Participants

Reaction Conditions

Reaction Steps

Alternatively, following General Procedure I, one-step Buchwald coupling, a microwave tube was charged with Xphos (0.1 equiv.), tris(dibenzylideneacetone)dipalladium(0) (0.05 equiv.), cesium carbonate (2 equiv.), 4-(2-chloro-8-((4-(2-methoxypropan-2-yl)piperidin-1-yl)methyl)-9-methyl-9H-purin-6-yl)morpholine (80 mg, 1 equiv.) and 2-methyl-1H-benzo[d]imidazole (1.2 equiv.). The vessel is evacuated and refilled with nitrogen prior to the addition of DMF or 1,4-dioxane. The mixture is heated in a microwave device, such as Biotage at about 140° C. for about 25-35 minutes. The reaction mixture is cooled to room temperature, filtered and concentrated, and purified by RP-HPLC to give 17.1 mg of 179. MS (Q1) 519.1 (M)+.

Provenance & Evidence