Pyrimidin-5-ol → 3-(Pyrimidin-5-yloxy)-4,5-dihydroisoxazole

Participants

Reaction Steps

3-(pyrimidin-5-yloxy)-4,5-dihydroisoxazole I-168a and I-168b were prepared in 2 steps from 1-(trifluoromethyl)-4-vinylbenzene using the cycloaddition conditions from Method 1. The resulting bromo-4,5-dihydroisoxazole was reacted with 5-hydroxypyrimidine to provide racemic compound I-168 using Method 5. These compounds can be separated using chiral HPLC methods known in the art. For example, see chiral HPLC Method disclosed herein. [M+H]+=309.8 m/z. Activity: B

Provenance & Evidence