Reacción #87927

Ecuación de reacción

{(4-cyano-2-methanesulfonyl-phenyl)-[6-oxo-2-(3-trifluoromethyl-phenylamino)-cyclohex-1-enyl]-methyl}-carbamic acid tert-butyl ester

INTERMEDIATE 16

{(4-cyano-2-methanesulfonyl-phenyl)-[6-oxo-2-(3-trifluoromethyl-phenylamino)-cyclohex-1-enyl]-methyl}-carbamic acid tert-butyl ester

hydrogen chloride

→

4-{Amino-[6-oxo-2-(3-trifluoromethyl-phenylamino)-cyclohex-1-enyl]-methyl}-3-methanesulfonyl-benzonitrile hydrochloride

Disolventes

1,4-dioxane

1,4-dioxane

tert-butylmethylether

Condiciones de reacción

Tratamiento posterior

1. 1
   Filtraciónthe precipitate is filtered off
2. 2
   Lavadowashed with tert-butylmethylether
3. 3
   Otrodried
4. 4
   Otro0.47 min (X012_S01)

Procedimiento

To a solution of {(4-cyano-2-methanesulfonyl-phenyl)-[6-oxo-2-(3-trifluoromethyl-phenylamino)-cyclohex-1-enyl]-methyl}-carbamic acid tert-butyl ester (INTERMEDIATE 16, 976 mg, 1.73 mmol) in 1,4-dioxane (2.0 mL) is added a solution of hydrogen chloride in 1,4-dioxane (4 M, 3.46 mL, 13.85 mmol) and the mixture is stirred at room temperature for 3 h. The reaction mixture is diluted with tert-butylmethylether and the precipitate is filtered off, washed with tert-butylmethylether and dried. Yield: 529 mg. ESI mass spectrum: [M+H]+=464; Retention time HPLC: 0.47 min (X012_S01).

Fuente