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1,2-Oxazol derivatives 3 were prepared by a highly regioselective 1,3-dipolar cycloaddition of nitrile oxides and α,β-acetylenicaldehydes 1 in good yields. Reactive nitrile oxides were generated in situ from stable chloro-oxime reagents 2 and triethyl amine. The cycloaddition reaction showed broad substrate scope and good functional group compatibility.
A formal [3+2] annulation reaction of 1,4-dithiane-2,5-diol and N-substituted imides through one-pot metal-free strategy has been developed. This method could furnish 2,3-thienoimides in good to high yields.
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