1,3,5-三取代吡唑的合成腈亚胺与偕二氮萘衍生的 Morita-Baylis-Hillman 碳酸酯的 1,3-偶极环加成反应。
Synthesis of 1,3,5-trisubstituted pyrazoles 1,3-dipolar cycloaddition of nitrile imines with ninhydrin-derived Morita-Baylis-Hillman carbonates.
机构信息
School of Pharmacy, Xinxiang University, Xinxiang 453000, P.R. of China.
Medical College, Xinxiang University, Xinxiang 453000, P.R. of China.
出版信息
Org Biomol Chem. 2022 Aug 31;20(34):6923-6930. doi: 10.1039/d2ob01253g.
PMID:35979893
Abstract
An effective synthetic method for 1,3,5-trisubstituted pyrazoles 1,3-dipolar cycloaddition reaction has been developed. This reaction could smoothly proceed between ninhydrin-derived Morita-Baylis-Hillman carbonates and nitrilimines to provide a wide scope of differently substituted pyrazoles in high yields (up to 95%). In addition, the reaction mechanism was also proposed to explain its regioselectivity.
摘要
发展了一种有效的 1,3,5-三取代吡唑的合成方法。该反应可以在由水合茚满衍生的 Morita-Baylis-Hillman 碳酸酯和亚胺之间顺利进行，以高产率（高达 95%）提供广泛的不同取代的吡唑。此外，还提出了反应机理来解释其区域选择性。
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