反应详情

(2-Chloro-4-morpholinopyrido[3,2-d]pyrimidin-6-yl)(4-(2-hydroxypropan-2-yl)piperidin-1-yl)methanone from Example 118 (80 mg) was reacted with 2-isopropyl-1H-benzo[d]imidazole (1.05 eq), sodium tert-butoxide (2 eq), palladium acetate (0.1 eq) and bis(tri-t-butylphosphine)palladium (0.1 eq). The tube was flushed with nitrogen for 10 minutes before adding Toluene (2 mL). The reaction was microwaved at 145° C. for 20 minutes. The crude was loaded onto a Biotage isolute scx-2 cartridge, eluted with 2M ammonia in MeOH then purified by flash column chromatography to afford 6.6 mg of 119. MS (Q1) 544.3 (M)+

1. customThe tube was flushed with nitrogen for 10 minutes
2. additionbefore adding Toluene (2 mL)
3. customThe reaction was microwaved at 145° C. for 20 minutes
4. washeluted with 2M ammonia in MeOH
5. customthen purified by flash column chromatography