isatoic anhydride

{{Chembox

| ImageFile = Isatoic anhydride.PNG

| ImageSize = 122 px

| ImageAlt =

| PIN = 2H-3,1-Benzoxazine-2,4(1H)-dione

| OtherNames =

|Section1={{Chembox Identifiers

| CASNo = 118-48-9

| ChEMBL = 346059

| ChemSpiderID = 8056

| DrugBank = DB11593

| EC_number = 204-255-0

| UNII_Ref = {{fdacite|correct|FDA}}

| UNII = R8TFA74Y4U

| CASNo_Ref = {{cascite|correct|CAS}}

| PubChem = 8359

| StdInChI=1S/C8H5NO3/c10-7-5-3-1-2-4-6(5)9-8(11)12-7/h1-4H,(H,9,11)

| StdInChIKey = TXJUTRJFNRYTHH-UHFFFAOYSA-N

| SMILES = C1=CC=C2C(=C1)C(=O)OC(=O)N2

}}

|Section2={{Chembox Properties

| C=8|O=3|H=5|N=1

| MolarMass =

| Appearance = white solid

| Density =

| MeltingPtC = 243

| BoilingPt =

| Solubility = }}

|Section3={{Chembox Hazards

| GHS_ref=[https://pubchem.ncbi.nlm.nih.gov/compound/8359#section=Safety-and-Hazards]

| GHSPictograms = {{GHS07}}

| GHSSignalWord = Warning

| HPhrases = {{H-phrases|317|319}}

| PPhrases = {{P-phrases|261|264+265|272|280|302+352|305+351+338|321|333+317|337+317|362+364|501}}

| MainHazards =

| FlashPt =

| AutoignitionPt = }}

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Isatoic anhydride is an organic compound derived from anthranilic acid. A white solid, it is prepared by reaction of anthranilic acid with phosgene.{{cite journal|journal=Org. Synth.|year=1947|volume=27|page=45|doi=10.15227/orgsyn.027.0045|title=Isatoic anhydride|author=E. C. Wagner |author2=Marion F. Fegley. }}

Reactions

Hydrolysis gives carbon dioxide and anthranilic acid. Alcoholysis proceeds similarly, affording the ester:

:C6H4C2O3NH + ROH → C6H4(CO2R)(NH2) + CO2

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.{{cite journal|title=The Chemistry of Isatoic Anhydride|author=Coppola, Gary M.|journal=Synthesis|year=1980|volume=7|issue=7 |pages=505–36|doi=10.1055/s-1980-29110}} 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{{cite journal | title = A survey of reported syntheses of methaqualone and some positional and structural isomers | author = Etienne F. van Zyl | journal = Forensic Sci. Int. | volume = 122 | pages = 142–149 | date = 2001 | issue = 2–3 | doi = 10.1016/S0379-0738(01)00484-4 | pmid = 11672968 }} 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

References