反应详情

温度

90 °C

A mixture of N-(1-(tert-butyldimethylsilyloxy)-2-methylpropan-2-yl)-2-(6-methyl-1H-indazol-3-yl)-5-trityl-5H-pyrrolo[3,2-b]pyrazine-7-carboxamide (200 mg, 0.277 mmol), 4-(2-chloroethyl)morpholine hydrochloride (62 mg, 0.333 mmol) and K2CO3 (191 mg, 1.385 mmol) in dry DMF (20 mL) was heated to 90° C. for 3 hours. Reaction mixture was extracted with ethyl acetate (100 mL), organic phase washed with water (3×10 mL) and brine (2×10 mL). The organic layer was dried over Na2SO4, filtered and concentrated to afford N-(1-(tert-butyldimethylsilyloxy)-2-methylpropan-2-yl)-2-(6-methyl-1-(2-morpholinoethyl)-1H-indazol-3-yl)-5-trityl-5H-pyrrolo[3,2-b]pyrazine-7-carboxamide (167 mg, crude) as a yellow oil. LCMS: (M+H)+=834.

1. customReaction mixture
2. extractionwas extracted with ethyl acetate (100 mL), organic phase
3. washwashed with water (3×10 mL) and brine (2×10 mL)
4. dry with materialThe organic layer was dried over Na2SO4
5. filtrationfiltered
6. concentrationconcentrated