Direct Lactamization of β-Arylated δ-Aminopentanoic Acid Carboxamides: En Route to 4-aryl-2-Piperidones, Piperidines, Antituberculosis Molecule Q203 (Telacebec) and its Analogues,Asian Journal of Organic Chemistry

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Direct Lactamization of β-Arylated δ-Aminopentanoic Acid Carboxamides: En Route to 4-aryl-2-Piperidones, Piperidines, Antituberculosis Molecule Q203 (Telacebec) and its Analogues
Asian Journal of Organic Chemistry ( IF 2.8 ) Pub Date : 2022-01-07 , DOI: 10.1002/ajoc.202100736
Radha Tomar ₁ , Debabrata Bhattacharya ₁ , Srinivasarao Arulananda Babu ₂

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Synthesis of medicinally important 4-aryl-2-piperidone, 4-arylpiperidine scaffolds, and antituberculosis molecule Q203 (Telacebec) was reported. Direct lactamization of β-C−H arylated δ-aminopentanoic acid carboxamides afforded 4-aryl-2-piperidones; which were converted into N-functionalized 4-aryl-2-piperidones, 4-arylpiperidines, and antituberculosis molecule Q203 and its analogues. The required β-C−H arylated carboxamides of δ-aminopentanoic acid were assembled using the Pd(II)-catalyzed C−H functionalization/arylation method.

中文翻译：

β-芳基化 δ-氨基戊酸甲酰胺的直接内酰胺化：通往 4-芳基-2-哌啶酮、哌啶、抗结核分子 Q203 (Telacebec) 及其类似物的过程

报道了具有药用价值的 4-芳基-2-哌啶酮、4-芳基哌啶支架和抗结核分子 Q203 (Telacebec) 的合成。β -C-H 芳基化δ-氨基戊酸甲酰胺的直接内酰胺化得到 4-芳基-2-哌啶酮；它们被转化为N-官能化的4-芳基-2-哌啶酮、4-芳基哌啶和抗结核分子Q203及其类似物。使用 Pd(II) 催化的 C-H 官能化/芳基化方法组装所需的δ-氨基戊酸的β -C-H 芳基化甲酰胺。

更新日期：2022-01-07

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