Trifluoroacetaldehyde N-tosylhydrazone in [3+2] cycloaddition reaction for the synthesis of 5-(trifluoromethyl)pyrazolinesстатья
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Аннотация:Trifl uoroacetaldehyde N-tosylhydrazone used as a precursor for the in situ generationof CF3CHN2 by treatment with weak bases in safe concentration underwent [3+2] cycloadditionto electron defi cient alkenes in the presence of N,N-diisopropylethylamine to give5-(trifl uoromethyl)pyrazolines in high yields. The reaction proceeded under mild conditions,tolerated a wide range of the substituents, and gave products promising for the drugdesign. The elaborated procedure avoided such drawbacks associated with the use ofCF3CHN2 as volatility, toxicity, and explosion hazard.