2-Substituted 3,3,3-trifluoroalanines, which have been little investigated, are highly selective, irreversible enzyme inhibitors. The new compounds 2 and 3 also belong to this class of molecules. The synthesis described here starts from oxazole 1, which is treated with an alkenyl or alkynyl alcohol, respectively, in the presence of KOH. Both 2 and 3 are capable of undergoing further functionalization. R1-R3 are, for example, CH3, C2H5, C2H3, H.
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Burger et al. (1988) studied this question.