Acylation of benzoxazolin-2-ones and 3-hydroxy-1,2-benzisoxazoles

Pol J Pharmacol Pharm. 1978 Sep-Oct;30(5):717-23.

Abstract

The acylation courses of 5-bromo and 5,7-dibromo derivatives of benzoxazolin-2--one (BO) and isomeric 3-hydroxy-1,2-benzisoxazoles (BIO) with acetic anhydride, benzoyl chlorides and alkyl chloroformates were investigated. In view of principal course of N-acylation in BO-and O-acylation in BIO-group some of the newly obtained compounds, namely 5,7-Br2-2-(o-chlorobenzoyloxy)-BO (5a) and N-alkoxycarbonyl BIO (22a--27a) make the exceptions. Compounds 25a and 26a were found to possess relatively the most intensive depressant action on the CNS.

MeSH terms

  • Acylation
  • Animals
  • Anticonvulsants
  • Benzoxazoles / chemical synthesis*
  • Benzoxazoles / pharmacology
  • Benzoxazoles / toxicity
  • Body Temperature / drug effects
  • Chemical Phenomena
  • Chemistry
  • Depression, Chemical
  • Isomerism
  • Isoxazoles / chemical synthesis*
  • Isoxazoles / pharmacology
  • Isoxazoles / toxicity
  • Lethal Dose 50
  • Mice
  • Oxazoles / chemical synthesis*

Substances

  • Anticonvulsants
  • Benzoxazoles
  • Isoxazoles
  • Oxazoles