1-Ethenyl-4-(trifluoromethyl)benzene → 3-(Pyridin-3-yloxy)-4,5-dihydroisoxazole

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Reaction Steps

3-(pyridin-3-yloxy)-4,5-dihydroisoxazole I-170a and I-170b were prepared in 3 steps from 1-(trifluoromethyl)-4-vinylbenzene using the cycloaddition conditions from Method 5. The resulting bromo-4,5-dihydroisoxazole was reacted with 5-hydroxypicolinic acid methyl ester using Method 5 followed by hydrolysis using the analogous conditions as in example 94. These compounds can be separated using chiral HPLC methods known in the art. For example, see chiral HPLC Method disclosed herein. [M+H]+=353.0 m/z. Activity: A

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