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Base Catalyzed Scaffold Shift from Pyranone Carboxamide to Pyrazolyl Acetamide through Intramolecular Ring Transformation

机译:碱催化的支架从吡喃酮羧酰胺到吡唑基乙酰胺通过分子内环转化

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摘要

Scaffold shift of biologically active pyranone carboxamide to pyrazolyl acetamide, which is another biologically important scaffold was achieved through one-pot base catalyzed metal- free intramolecular ring transformation. Out of the two probable mechanistic pathways (Figure 3), substitution at C-4 by hydrazineyl leading to a pyranone intermediate followed by an intramolecular attack of hydrazineyl at C-6 and decarbox- ylation to yield pyrazolyl acetamides was rationalized through LCMS, UV monitoring and computational studies.
机译:生物活性吡喃酮羧酰胺向吡唑基乙酰氨酰胺的脚手架移位,这是另一个具有生物学上重要的支架,通过一锅碱催化金属 - 无分子内环转化实现。 在两种可能的机械途径中(图3),在C-4上用羟基氨基取代,导致吡喃酮中间体,然后在C-6处丝氨酸内分子内攻击,并产生脱碳二碳二烯基并产生通过LCMS的吡唑基乙酰胺,UV监测,UV监测 和计算研究。

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