Réaction #4276

Équation de réaction

1-methyl-2-chloromethyl-5-(2'-fluorophenyl)-2,3-dihydro-1H-1,4-benzodiazepine

m-trifluoromethyl aniline

potassium carbonate

sodium iodide

→

1-methyl-2-(3'-trifluoromethylphenyl)aminomethyl-5-(2'-fluorophenyl)-2,3-dihydro-1H-1,4-benzodiazepine

Solvants

N,N-dimethylformamide

Conditions de réaction

Traitement

1. 1
   AutreAfter solvent-removal
2. 2
   Autrepartitioning
3. 3
   Autreseparation
4. 4
   Lavagewashing
5. 5
   Autredrying
6. 6
   Concentrationconcentrating
7. 7
   Autrethe analytical product was obtained via chromatography on silica gel (ethyl acetate-hexane elution, 3:7 v/v)

Mode opératoire

According to the method of Example 5, 1-methyl-2-chloromethyl-5-(2'-fluorophenyl)-2,3-dihydro-1H-1,4-benzodiazepine (200 mg, 0.66 mmole) and m-trifluoromethyl aniline (319 mg, 1.97 mmole) were combined in 2 ml of dry N,N-dimethylformamide, and potassium carbonate (273 mg, 1.97 mmole) and sodium iodide (198 mg, 1.32 mmole) were added to this mixture (which was heated at 65° C. for 18 hours). After solvent-removal, partitioning, separation, washing, drying and concentrating, the analytical product was obtained via chromatography on silica gel (ethyl acetate-hexane elution, 3:7 v/v) and was shown to be 96% pure by HPLC.

Source