Reacción #167805

Ecuación de reacción

(8S)-2-morpholin-4-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one

tripotassium phosphate

(1S,2S)-cyclo-hexane-1,2-diamine

1-iodo-3-methylbenzene

→

(8S)-9-(3-methylphenyl)-2-(morpholin-4-yl)-8-(trifluoro-methyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one

Disolventes

dimethylformamide

CH2Cl2 MeOH

CH2Cl2

Condiciones de reacción

Tratamiento posterior

1. 1
   OtroThe product is prepared
2. 2
   Otroare obtained in the form of a green solid

Procedimiento

The product is prepared according to the procedure described in Example 12, but using 250 mg of (8S)-2-morpholin-4-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one (Example 1e) in 4 ml of dimethylformamide, 251 mg of 1-iodo-3-methylbenzene, 349 mg of tripotassium phosphate, 156 mg of copper iodide and 93 mg of (1S,2S)-cyclo-hexane-1,2-diamine. After 1 hour at 150° C. under microwave irradiation and silica column purification of the resulting reaction mixture (elution gradient of CH2Cl2 to CH2Cl2/MeOH 98/02), 195 mg of (88)-9-(3-methylphenyl)-2-(morpholin-4-yl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]-pyrimidin-4-one are obtained in the form of a green solid, the characteristics of which are the following:

Fuente