反应详情

温度

30 °C

A mixture of 1H-indazol-4-ylboronic acid (0.2 g, 1.227 mmol), chloromethyl pivalate (554 mg, 3.68 mmol) and K2CO3 (509 mg, 3.68 mmol) in dry DMF (10 mL) was heated to 30° C. for 16 hours. Reaction was quenched with water and product extracted with ethyl acetate (150 mL), then washed with water (3×20 mL) and brine (2×20 mL), then dried over Na2SO4, filtered and concentrated. The product (114 mg, crude) was obtained and used into next step without further purification. LCMS: (M+Na)+=299.

1. customReaction
2. customwas quenched with water and product
3. extractionextracted with ethyl acetate (150 mL)
4. washwashed with water (3×20 mL) and brine (2×20 mL)
5. dry with materialdried over Na2SO4
6. filtrationfiltered
7. concentrationconcentrated
8. customThe product (114 mg, crude) was obtained
9. customused into next step without further purification