Isatoic anhydride


Isatoic anhydride is an organic compound derived from anthranilic acid. A white solid, it is prepared by reaction of anthranilic acid with phosgene.

Reactions

Hydrolysis gives carbon dioxide and anthranilic acid. Alcoholysis proceeds similarly, affording the ester:
Amines also effect ring-opening. Active methylene compounds and carbanions replace oxygen giving hydroxyquinolinone derivatives. Deprotonation followed by alkylation gives the N-substituted derivatives. Sodium azide gives the benzimidazolone via the isocyanate. Isatoic anhydride is used as a blowing agent in the polymer industry, an application that exploits its tendency to release CO2.

Uses

Isatoic anhydride has been used as a precursor for the synthesis of methaqualone and related 4-quinazolinone-based pharmaceutical drugs, including:
  1. Tioperidone
  2. Tranilast
  3. Pelanserin
  4. Diproqualone
  5. Antrafenine
  6. SJ-733
  7. Nicafenine
  8. Molinazone
  9. Cloperidone
  10. SGB 1534