Réaction #792170

Équation de réaction

benzoxazinone

2-[3-Bromo-1-(3-chloro-2-pyridinyl)-1H-pyrazol-5-yl]-6-chloro-8-methyl-4H-3,1-benzoxazin-4-one

methylamine

→

title compound

3-Bromo-N-[4-chloro-2-methyl-6-[(methylamino)carbonyl]phenyl]-1-(3-chloro-2-pyridinyl)-1H-pyrazole-5-carboxamide

Solvants

tetrahydrofuran

Conditions de réaction

Traitement

1. 1
   Températurecooled to room temperature
2. 2
   AutreThe tetrahydrofuran solvent was evaporated under reduced pressure
3. 3
   Autrethe residual solid was triturated with ether
4. 4
   Filtrationfiltered
5. 5
   Autredried

Mode opératoire

To a solution of the benzoxazinone product of Example 10, Step E (0.20 g, 0.44 mmol) in tetrahydrofuran was added methylamine (2.0 M solution in THF, 0.514 mL, 1.02 mmol), and the reaction mixture was heated to 60° C. for 90 minutes and then cooled to room temperature. The tetrahydrofuran solvent was evaporated under reduced pressure, and the residual solid was triturated with ether, filtered, and dried to afford the title compound, a compound of the present invention, as a solid (40 mg), m.p. 162-164° C.

Source