反应详情

(6-Bromopyridin-2-yl)acetic acid (Example 235, Step 2) (41% wt, 1.50 g, 2.85 mmol), EDC (1.64 g, 8.54 mmol), HOBT (872 mg, 5.69 mmol), and cyclopropanecarboxylic acid hydrazide (570 mg, 5.69 mmol) were combined in DMF (15 mL), and DIEA (994 μL, 5.69 mmol) was added. The reaction was stirred overnight at room temperature. After evaporation of the DMF, the residue was diluted with water and extracted with 5:1 CH2Cl2:MeOH (3×). The combined organic layers were dried (MgSO4), filtered, and evaporated. The solid residue was triturated with CH2Cl2 and filtered to isolate the title compound as a colorless solid.

1. customAfter evaporation of the DMF
2. additionthe residue was diluted with water
3. extractionextracted with 5:1 CH2Cl2
4. dry with materialThe combined organic layers were dried (MgSO4)
5. filtrationfiltered
6. customevaporated
7. customThe solid residue was triturated with CH2Cl2
8. filtrationfiltered