• Media type: E-Article
  • Title: Cyclization reactions of tricarbonylmethane thiosemicarbazones: Formation of 1,3,4‐thiadiazole derivatives with concomitant CC bond cleavage
  • Contributor: Somogyi, László
  • imprint: Wiley, 1995
  • Published in: Liebigs Annalen
  • Language: English
  • DOI: 10.1002/jlac.1995199504107
  • ISSN: 0947-3440
  • Keywords: General Chemistry
  • Origination:
  • Footnote:
  • Description: <jats:title>Abstract</jats:title><jats:p>Under acylating conditions 3‐acetyl‐4‐hydroxy‐2<jats:italic>H</jats:italic>‐pyran‐2‐one thiosemicarbazones (<jats:bold>1a, b</jats:bold> and <jats:bold>2a, b</jats:bold>) are transformed into 2‐(acylamino)‐5‐methyl‐1,3,4‐thiadiazoles <jats:bold>3b, c, e, f</jats:bold> and 2<jats:italic>H</jats:italic>‐pyran‐2‐ones <jats:bold>1c</jats:bold> and <jats:bold>2c</jats:bold> via C–C bond cleavage. Similarly, the reaction of <jats:bold>1b</jats:bold> with RCO<jats:sub>2</jats:sub>H/EtOH (R = Me, Et) affords 2‐anilino‐5‐methyl‐1,3,4‐thiadiazole (<jats:bold>3d</jats:bold>) and triacetic acid lactone <jats:bold>1c.</jats:bold> Upon treatment with Ac<jats:sub>2</jats:sub>O/Et<jats:sub>3</jats:sub>N the dehydroacetic acid derivative <jats:bold>1b</jats:bold> is transformed into the thiadiazoline <jats:bold>4</jats:bold>, while the benzo derivative <jats:bold>2b</jats:bold> is converted into thiadiazole <jats:bold>3e</jats:bold> and 4‐acetoxycoumarin (<jats:bold>2c</jats:bold>).</jats:p>