反应详情

A suspension of 3-(3-fluorophenyl)-1-(6,7,8,9-tetrahydro-5H-cyclohept[d]imidazo[2,1-b]thiazol-3-yl)-2-propene-1-one (Formula N-6, X=3-fluoro), 1.02 g, in THF (100 mL) at −78° was treated with LiAlH4 (0.27 g) and reacted for 18 hours. The mixture was then maintained at −20° for 24 hours and excess reagent was quenched. The mixture was filtered, the filtrate was concentrated, the residue was dissolved in ethyl acetate, washed with saline, dried and evaporated. The residue (0.30 g) was crystallized from acetonitrile to yield pure α-[2-(3-fluorophenyl) ethyl]-6,7,8,9-tetrahydro-5H-cyclohept[d]imidazo[2,1-b]thiazol-3-methanol, 0.21 g (m.p. 141-144°), Formula N-7, X=3-fluoro.

1. customreacted for 18 hours
2. temperatureThe mixture was then maintained at −20° for 24 hours
3. customexcess reagent was quenched
4. filtrationThe mixture was filtered
5. concentrationthe filtrate was concentrated
6. dissolutionthe residue was dissolved in ethyl acetate
7. washwashed with saline
8. customdried
9. customevaporated
10. customThe residue (0.30 g) was crystallized from acetonitrile