Реакция #792170

Уравнение реакции

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

Растворители

tetrahydrofuran

Условия реакции

Обработка

1. 1
   Температураcooled to room temperature
2. 2
   ДругоеThe tetrahydrofuran solvent was evaporated under reduced pressure
3. 3
   Другоеthe residual solid was triturated with ether
4. 4
   Фильтрацияfiltered
5. 5
   Другоеdried

Методика

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.

Источник