(equation presented) The preparation of novel isoxazolocyclobutanone and isoxazolinocyclobutenone derivatives via a traceless solid-phase sulfone linker strategy is described. Key steps in the solid-phase protocol reported here include (i) sulfinate → sulfone alkylation, (ii) four-member ring formation by sulfone dianion alkylation, (iii) heterocycle formation by nitrile oxide 1,3-dipolar cycloaddition, and (iv) traceless product release by cyclobutanol → cyclobutanone oxidation with concomitant linker cleavage by sulfinate elimination.
|Original language||English (US)|
|Number of pages||4|
|State||Published - Mar 7 2002|
ASJC Scopus subject areas
- Molecular Medicine