Sulfonyl derivatives of benzotriazole: Part 1. A novel approach to the activation of carboxylic acids

1-Acylbenzotriazoles are prepared from 1-(1-methanesulfonyl)benzotriazole and carboxylic acids as illustrated by the preparation of 1-(2-pyridoyl)-, 1-(3-pyridoyl)-, 1-(4-pyridoyl)-, 1-(2-pyrrolylcarbonyl)- and 1-(2-furoyl)-benzotriazole in yields of 80 – 95%.

Alan R. Katritzky

2002

Scholarcy highlights

  • 1-Acylbenzotriazoles are prepared from 1-(1-methanesulfonyl)benzotriazole and carboxylic acids as illustrated by the preparation of 1-(2-pyridoyl)-, 1-(3-pyridoyl)-, 1-(4-pyridoyl)-, 1-(2-pyrrolylcarbonyl)- and 1-(2-furoyl)-benzotriazole in yields of 80 – 95%.
  • 1-Acylbenzotriazoles are prepared in good yields by fusion of benzotriazole and acid chlorides at 80 – 100°C.
  • In cases when the corresponding acid chlorides are not available, 1-acylbenzotriazoles are conveniently available from 1-(1-methanesulfonyl)benzotriazole and the respective carboxylic acids as illustrated by the preparation of 2-, 3-, and 4-pyridoyl-, 2-pyrrolylcarbonyl- and 2-furoyl-benzotriazole in yields of 80 – 95%.
  • Preparations of two sulfonyl derivatives of benzotriazole are described.

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