反应详情

To thiourea (1.77 g, 23.3 mmol) in water (50 ml) was added 1-chloro-3-(2-fluoro-4-biphenylyl)-2-butanone (5.25 g, 19.0 mmol). After addition, the mixture was heated for 3 hr, and the solution was cooled to room temperature, then added IN sodium hydroxide to pH 8. The mixture was extracted with chloroform and the chloroform extracts were washed with water, dried over, and evaporated under reduced pressure to a residue, which was chromatographed to afford 2-amino-4-[1-(2-fluoro-4-biphenylyl)ethyl] thiazole (4.12 g, 73% yield) as crystalline material: mp 167°-168° C.

1. additionAfter addition
2. temperaturethe mixture was heated for 3 hr
3. extractionThe mixture was extracted with chloroform
4. washthe chloroform extracts were washed with water
5. customdried over, and
6. customevaporated under reduced pressure to a residue, which
7. customwas chromatographed