反应详情

A stirred solution of (5-methyl-3-phenyl-4-isoxazolyl)methylamine (100 mg, 0.53 mmol) and 2-chloro-thiazole-5-carboxylic acid isopropylamide (100 mg, 0.49 mmol) in DMF (5 mL) was heated at 100° C. for 7 days, then at 150° C. under microwave irradiation for 15 min. The reaction mixture was cooled and concentrated in vacuo, then diluted with water and extracted with ethyl acetate. The combined organic extracts were dried, filtered and concentrated, then purified by chromatography (silica, 0 to 3% methanol in dichloromethane) to give the title compound (23 mg, 12%) as a white solid. MS: m/e=357.3 [M+H]+.

1. customat 150° C. under microwave irradiation for 15 min
2. temperatureThe reaction mixture was cooled
3. concentrationconcentrated in vacuo
4. additiondiluted with water
5. extractionextracted with ethyl acetate
6. customThe combined organic extracts were dried
7. filtrationfiltered
8. concentrationconcentrated
9. custompurified by chromatography (silica, 0 to 3% methanol in dichloromethane)