Reacción #92251

Ecuación de reacción

(R)-5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidine

nitric acid

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product

Rendimiento 58.0%

(R)-5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)-3-nitropyrazolo[1,5-a]pyrimidine

Rendimiento 58.0%

Disolventes

TFA

Condiciones de reacción

Tratamiento posterior

1. 1
   Otroto give a clear yellowish solution
2. 2
   workup.ADDITIONAfter addition
3. 3
   Otroquenched
4. 4
   workup.ADDITIONby pouring onto ice with rapid stirring
5. 5
   FiltraciónThe resulting yellowish suspension was filtered
6. 6
   Lavadorinsed with water
7. 7
   Otrothe solid was triturated with MeOH (50 mL, with brief sonication)
8. 8
   Filtraciónvacuum-filtered

Procedimiento

(R)-5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidine (3.3 g, 10.99 mmol), was dissolved in 25 mL TFA at ambient temperature to give a clear yellowish solution, then nitric acid (3.434 mL, 54.94 mmol) was added drop-wise to the solution with rapid stirring. After addition, the reaction mixture was stirred for another 15 minutes at ambient temperature, then quenched by pouring onto ice with rapid stirring. The resulting yellowish suspension was filtered, rinsed with water, then the solid was triturated with MeOH (50 mL, with brief sonication), and vacuum-filtered, giving the pure product as a fine off-white powder (2.2 g, 58% yield).

Fuente