Reacción #332740

Ecuación de reacción

tert-butyl 6,7-difluoro-5-formyl-1,2-benzisoxazol-3-yl carbonate

531

tert-butyl 6,7-difluoro-5-formyl-1,2-benzisoxazol-3-yl carbonate

barbituric acid

IPA

→

tert-butyl (2R,4S,4aS)-rel-11-fluoro-2,4-dimethyl-2′,4′,6′-trioxo-1,1′,2,3′,4,4′,4a,6′-octahydro-2′H,6H-spiro[isoxazolo[4,5-g][1,4]oxazino[4,3-a]quinoline-5,5′-pyrimidin]-8-yl carbonate

Condiciones de reacción

Tratamiento posterior

1. 1
   OtroSolvents were evaporated
2. 2
   Otrothe residue was purified over a silica gel column
3. 3
   Otroto give product as a white solid

Procedimiento

To a stirred solution of tert-butyl 6,7-difluoro-5-formyl-1,2-benzisoxazol-3-yl carbonate Intermediate 531 (175 mg, 0.44 mmol) in dry IPA (10 mL) was added barbituric acid (8 mg, 0.062 mmol), and the solution heated around 80° C. for 12 h. Solvents were evaporated and the residue was purified over a silica gel column to give product as a white solid. Yield: 40 mg (18%).

Fuente