反应详情

To a solution of (R)-5-(4-(morpholine-4-carbonyl)phenylamino)-3-(piperidin-3-ylamino)-1,2,4-triazine-6-carboxamide (75) HCl salt (60 mg, 0.13 mmol) in NMP (3 mL) was added DIEA (90 μL, 0.76 mmol) and then 4-tert-butylbenzoyl chloride (39 mg, 0.20 mmol). The mixture was stirred at RT for 20 min, quenched with TFA (0.1 mL), diluted with 2 mL water, and subjected to reverse phase preparative HPLC to afford the title compound (76) as an HCl salt. MS found for C31H38N8O4 as (M+H)+ 587.2, (M−H)− 585.2. UV: λ=268, 287 nm.

1. customquenched with TFA (0.1 mL)
2. additiondiluted with 2 mL water