反应详情

温度

50 °C

Ethanolamine (1 mL) was added to N-cyclopropyl-4-methyl-3-{3-[(1-{2-[(2R)-oxiran-2-ylmethoxy]phenyl}cyclopropyl)amino]-2-oxopyrazin-1(2H)-yl}benzamide (Example 299a, 7.81 g) in DMF (3 mL). The reaction was heated at 50° C. overnight. The reaction mixture was partitioned between water and DCM. The combined organics were dried (MgSO4), filtered and evaporated. Purification by preparative HPLC (Xbridge column, eluting with a gradient of acetonitrile in 0.2% (v/v) aqueous ammonia) gave the title product (0.102 g) after solvent removal and trituration with diethyl ether.

1. customThe reaction mixture was partitioned between water and DCM
2. dry with materialThe combined organics were dried (MgSO4)
3. filtrationfiltered
4. customevaporated
5. customPurification by preparative HPLC (Xbridge column
6. washeluting with a gradient of acetonitrile in 0.2% (v/v) aqueous ammonia)