A novel idea of sulfamic acid as an efficient catalyst for the synthesis of 2-azapyrrolizidine derivatives

IF 0.9 Q4 CHEMISTRY, PHYSICAL Current Organocatalysis Pub Date : 2022-07-28 DOI:10.2174/2213337209666220728114131
R. Tafer, R. Boulcina, A. Debache
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引用次数: 0

Abstract

The synthesis of 2-azapyrrolizidine scaffolds has fascinated scientists due to their potential biological activities. An efficient and environmentally sustainable synthetic method has been presented to synthesize structurally various 2-azapyrrolizidines via three-component reaction. The condensation of aldehydes, hydantoin, and malononitrile in the presence of green and sustainable sulfamic acid as catalyst in mild conditions has been achieved. The present protocol leads in most cases to the desired products in high yields. The synthetic efficiency and operational simplicity make the present procedure cost effective, time efficient and eco-friendly for the synthesis of substituted 2-azapyrrolizidines.
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氨基磺酸作为高效催化剂合成2-氮杂吡咯烷衍生物的新思路
2-氮杂吡咯利西啶支架的合成因其潜在的生物活性而引起了科学家们的兴趣。提出了一种高效、环保的三组分合成方法,可合成结构多样的2-氮杂吡咯里嗪类化合物。在绿色和可持续的氨基磺酸作为催化剂的存在下,在温和的条件下实现了醛、乙酰英和丙二腈的缩合。目前的方案在大多数情况下都能获得高产量的所需产品。该方法的合成效率高,操作简单,具有成本效益、时间效率和环境友好性,可用于取代2-氮杂吡咯里嗪的合成。
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来源期刊
Current Organocatalysis
Current Organocatalysis CHEMISTRY, PHYSICAL-
CiteScore
2.00
自引率
0.00%
发文量
28
期刊介绍: Current Organocatalysis is an international peer-reviewed journal that publishes significant research in all areas of organocatalysis. The journal covers organo homogeneous/heterogeneous catalysis, innovative mechanistic studies and kinetics of organocatalytic processes focusing on practical, theoretical and computational aspects. It also includes potential applications of organocatalysts in the fields of drug discovery, synthesis of novel molecules, synthetic method development, green chemistry and chemoenzymatic reactions. This journal also accepts papers on methods, reagents, and mechanism of a synthetic process and technology pertaining to chemistry. Moreover, this journal features full-length/mini review articles within organocatalysis and synthetic chemistry. It is the premier source of organocatalysis and synthetic methods related information for chemists, biologists and engineers pursuing research in industry and academia.
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