反应详情

To a stirred solution of 0.1 g (0.49 mmol) (2-amino-thiophen-3-yl)-phenyl-methanone (the preparation of which is described in example 20) in 10 ml dichloromethane at 0° C. was added 68 mg (0.49 mmol) N-chloro-succinimide (NCS). The mixture was then stirred from 0° C. to RT over night, and then poured onto water and extracted three times with ethyl acetate. The combined organic phases were dried over sodium sulfate and concentrated in vacuo. Flash chromatography (heptane/ethyl acetate 3:1) afforded 40 mg (34%) (2-amino-5-chloro-thiophen-3-yl)-phenyl-methanone as a yellow solid.

1. customat 0° C.
2. additionpoured onto water
3. extractionextracted three times with ethyl acetate
4. dry with materialThe combined organic phases were dried over sodium sulfate
5. concentrationconcentrated in vacuo