PDF(Pubmed)
Abstract：
The enantioselective 1,4-addition reaction of pyrazolin-5-ones to α,β-unsaturated ketones catalyzed by a cinchona alkaloid-derived primary amine-Brønsted acid composite is reported. Both enantiomers of the anticipated pyrazole derivatives were obtained in good to excellent yields (up to 97%) and high enantioselectivities (up to 98.5% ee) under mild reaction conditions. In addition, this protocol was further expanded to synthesize highly enantioenriched hybrid molecules bearing biologically relevant heterocycles.
摘要：
吡唑啉-5-酮与α的对映选择性1,4-加成反应，据报道，由金鸡纳生物碱衍生的伯胺-布朗斯台德酸复合材料催化的β-不饱和酮。在温和的反应条件下，以良好至优异的产率（高达97％）和高对映选择性（高达98.5％ee）获得了预期的吡唑衍生物的两种对映体。此外,该方案进一步扩展到合成具有生物相关杂环的高度对映体富集的杂化分子。
