反应详情

温度

100 °C

To a solution of 2-amino-3,4,6-trifluorothiophenol (1.79 g, 10 mmol) in NMP (5 ml) was added dropwise a solution of succinic anhydride (1.0 g, 10 mmol) in NMP (5 ml) at ambient temperature under a nitrogen stream and the mixture was heated to 100° C. for 1 hour. The resultant mixture was basified by dilution with aqueous sodium carbonate and washed with ether. The aqueous layer was acidified with 7% hydrochloric acid and extracted with ethyl acetate. The organic layer was washed with water, then dried and evaporated to yield crude crystals, which were washed with hexane-isopropyl ether to give 3-(4,5,7-trifluorobenzothiazol-2-yl)propionic acid 2.16 g, 83%).

1. washwashed with ether
2. extractionextracted with ethyl acetate
3. washThe organic layer was washed with water
4. customdried
5. customevaporated
6. customto yield crude crystals, which
7. washwere washed with hexane-isopropyl ether