合成α,β-不饱和炔酰胺的新途径

A New Method for the Synthesis of α,β-Acetylenic Amides

α,β-不饱和炔酰胺是有用的合成中间体,它们通常是由其相应的羧酸衍生物与胺反应制得。我们在应用Weyerstahl的方法从乙酰乙酸乙酯(1)制备丁炔一2一酸(5)时。

A new synthetic method of a, β-acetylenic amides was accomplished by NH_3, pri- mary and secondary amineinduced ring-0pening of 4,4-dibromo-3-methyl-2-pyrazoline-5- one (4). This method has been applied to the syntheses of ten a,β-acetylenic amides (6) which were characterized by ~1H NMR, IR, MS, HRMS spectra and elemental analyses.