反应详情

To a mixture of 2,6-dichloro-5-cyclopropylnicotinamide (2.00 g, 8.66 mmol) and 5-hydroxypentan-2-one (883 mg, 8.66 mmol) in DMF (30 mL) was added and NaH (416 mg, 10.4 mmol) in portions at 0° C. The mixture was stirred at r.t. overnight, quenched by water, extracted by EtOAc. The separated organics was dried, concentrated and purified by column chromatography (Petroleum ether:EtOAc=10:1˜1:1) to give 6-chloro-5-cyclopropyl-2-(4-oxopentyloxy)nicotinamide (500 mg, 19.4%).

1. additionwas added
2. customat 0° C
3. customquenched by water
4. extractionextracted by EtOAc
5. customThe separated organics was dried
6. concentrationconcentrated
7. custompurified by column chromatography (Petroleum ether:EtOAc=10:1˜1:1)