Potassium Phosphate, Tribasic → 4-(8-amino-3-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)imidazo [1,5-a]pyrazin-1-yl)-N-(4-isopropoxypyridin-2-yl)benzamide

Participants

Reaction Conditions

Reaction Steps

A seal 4 ml vial containing N-(4-isopropoxypyridin-2-yl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzamide, (31.3 mg, 0.082 mmol), 1-bromo-3-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)imidazo[1,5-a]pyrazin-8-amine, (30 mg, 0.074 mmol), and 2nd Generation Xphos Precatalyst (11.71 mg, 0.015 mmol) was treated with Dioxane (372 μl) via a syringe and needle. The resulting suspension was then degassed with house vacuum and back filled with N2. Potassium phosphate tribasic (112 μl, 0.223 mmol) was then added via a syringe and needle and the resulting cream suspension stirred at 60° C. for 5 h. Purification on the Mass Directed HPLC (method: 5 to 35% MeCN/Water w/0.05% TFA on a 30 mm×100 mm, 5 m Waters SunFire RP C-18 Column) afforded 8 mg of the Title compound as a yellow solid/LC-MS (M+1) 579.39.

Provenance & Evidence