TREA

Coupling process for preparing quinolone intermediates

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Information

  • Patent Application
  • 20070232804
  • Publication Number
    20070232804
  • Date Filed
    March 26, 2007
    19 years ago
  • Date Published
    October 04, 2007
    18 years ago
Information
Abstract
Process for making 7-cycloamino-1-cyclopropyl-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acids. Borate ester compounds suitable for use in such process.
Description
Claims
  • 1. A process for preparing a substituted quinolone according to Formula I:
  • 2. A process according to claim 1, wherein R1 is methyl.
  • 3. A process according to claim 1, wherein R2 is cyclopropyl.
  • 4. A process according to claim 1, wherein R4 is methyl.
  • 5. A process according to claim 1, wherein R3 is acetoxy.
  • 6. A process according to claim 1, wherein R5 is amino.
  • 7. A process according to claim 1, wherein R5 is amino-tert-butoxycarbonyl.
  • 8. A process according to claim 7, wherein the resulting compound of Formula I is subsequently subjected to a process of deprotecting the amino group of R5.
  • 9. A process according to claim 1, wherein the quinolone of Formula I is:
  • 10. A process according to claim 1, wherein the compound of Formula III is:
  • 11. A process according to claim 1, wherein the compound of Formula II is:
  • 12. A process according to claim 1, wherein the base is selected from the group consisting of triethylamine, diisopropylethylamine, triisopropyl amine, and 1,8-diazabicyclo[5.4.0]undec-7-ene.
  • 13. A process according to claim 12, wherein the base is triethylamine.
  • 14. A compound having the structure:
Provisional Applications (1)
Number Date Country
60786482 Mar 2006 US