Synthesis p. 439 - 442 (1997)
Update date:2022-07-30
Topics:
Bunnelle
Singam
Narayanan
Bradshaw
Liou
A concise, regiocontrolled route to isoxazoles, based on the condensation of an ester with a metallated imine, has been developed. The intermediate vinylogous amides react smoothly with hydroxylamine to provide, after dehydration, substituted isoxazoles. The method has been used for the multi-kilo scale preparation of ABT-418, a novel cholinergic channel activator.
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