Reacción #1732117

Ecuación de reacción

(S)-3-(hydroxymethyl)-7,8,9,10-tetrahydro-5H-dipyrido[1,2-a:3′,2′-e]pyrazin-6(6aH)-one

(cyanomethyl)trimethylphosphonium iodide

DIEA

N-ethyl-4-(piperazin-1-yl)benzamide

→

(S)-N-ethyl-4-(4-((6-oxo-6,6a,7,8,9,10-hexahydro-5H-dipyrido[1,2-a:3′,2′-e]pyrazin-3-yl)methyl)piperazin-1-yl)benzamide

Condiciones de reacción

Tratamiento posterior

1. 1
   OtroThe crude reaction
2. 2
   Temperaturawas cooled to RT
3. 3
   Filtraciónfiltered
4. 4
   OtroThe resulting solid were collected
5. 5
   Temperaturaheated
6. 6
   Temperaturato reflux
7. 7
   Temperaturacooled to RT
8. 8
   Filtraciónfiltered
9. 9
   LavadoThe resulting material was rinsed with EtOH
10. 10
    Otroto give a white solid

Procedimiento

To a suspension of (S)-3-(hydroxymethyl)-7,8,9,10-tetrahydro-5H-dipyrido[1,2-a:3′,2′-e]pyrazin-6(6aH)-one (800 mg, 3.43 mmol) was added (cyanomethyl)trimethylphosphonium iodide (1000 mg, 4.12 mmol) and DIEA (1797 μl, 10.29 mmol) and N-ethyl-4-(piperazin-1-yl)benzamide (800 mg, 3.43 mmol)). The vial was heated to 90° C. for 16 hours. The crude reaction was cooled to RT and filtered. The resulting solid were collected and suspended in EtOH (24 mL), heated to reflux, then cooled to RT and filtered. The resulting material was rinsed with EtOH to give a white solid.

Fuente