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- W4205952648 abstract "Abstract We report the synthesis of 4‐aryl‐2‐piperidone, 4‐arylpiperidine motifs, antituberculosis molecule Q203 (Telacebec) and its analogues. Direct lactamization of β ‐C−H arylated N ‐phthaloyl δ ‐aminopentanoic acid carboxamides yielded 4‐aryl‐2‐piperidone (4‐aryl‐ δ ‐valerolactam) scaffolds. The required β ‐C−H arylated N ‐phthaloyl δ ‐aminopentanoic acid carboxamides were assembled via the Pd(II)‐catalyzed, 8‐aminoquinoline‐aided, sp 3 β ‐C−H activation and arylation method. The β ‐C−H arylated N ‐phthaloyl δ ‐aminopentanoic acid carboxamides containing both 8‐aminoquinoline and N ‐phthaloyl protecting groups directly underwent the hydrazine‐mediated lactamization to afford 4‐aryl‐2‐piperidones. 4‐Aryl‐2‐piperidone scaffolds were then converted into N ‐functionalized 4‐aryl‐2‐piperidones, 4‐arylpiperidines, which are structurally closer to bio‐active 4‐aryl‐ 2‐piperidone and piperidine motifs. A synthetic route for assembling antituberculosis molecule Q203 and its analogues from the corresponding 4‐aryl‐2‐piperidones was also shown." @default.
- W4205952648 created "2022-01-25" @default.
- W4205952648 creator A5038086935 @default.
- W4205952648 creator A5061409016 @default.
- W4205952648 creator A5065453343 @default.
- W4205952648 date "2022-01-30" @default.
- W4205952648 modified "2023-10-16" @default.
- W4205952648 title "Direct Lactamization of <i>β</i>‐Arylated <i>δ</i>‐Aminopentanoic Acid Carboxamides: En Route to 4‐aryl‐2‐Piperidones, Piperidines, Antituberculosis Molecule Q203 (Telacebec) and its Analogues" @default.
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