ChemInform Abstract: Synthesis of Partially Saturated Condensed Triazoles by Reaction of . omega.‐Aminoalkyl‐1,2,4‐triazoles with Electrophiles.

Abstract

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4-(3-Chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-methoxypyridin-2-yl)piperazine-1-carbothioamide (ML267), a Potent Inhibitor of Bacterial Phosphopantetheinyl Transferase That Attenuates Secondary Metabolism and Thwarts Bacterial Growth

“…21−24 Phenoxycarbonyl chloride-assisted coupling of 1-(3-(trifluoromethyl)phenyl)piperazine with 4-picolin-2-amine afforded the urea analogue 12 . Analogue 13 was prepared by stirring the analogue 1 with ammonium hydroxide and sodium periodate at 80 °C in a DMF–water solvent mixture.…”

“…Through bioisosteric replacement of the thiourea, analogues 12–17 were synthesized utilizing known protocols reported for similar compounds in the literature as shown in Scheme (see the Supporting Information for details). − Phenoxycarbonyl chloride-assisted coupling of 1-(3-(trifluoromethyl)­phenyl)­piperazine with 4-picolin-2-amine afforded the urea analogue 12 . Analogue 13 was prepared by stirring the analogue 1 with ammonium hydroxide and sodium periodate at 80 °C in a DMF–water solvent mixture.…”