Reacción #48761

Ecuación de reacción

triethyl amine

acetic anhydride

5-[2-amino-3-(3-fluoro-5-propoxy-phenyl)-1-hydroxy-propyl]-2-(3-fluoro-2-fluoromethyl-2-methyl-propoxy)-3-methyl-morpholine-4-carboxylic acid tert-butyl ester

→

5-[2-acetylamino-3-(3-fluoro-5-propoxy-phenyl)-1-hydroxy-propyl]-2-(3-fluoro-2-fluoromethyl-2-methyl-propoxy)-3-methyl-morpholine-4-carboxylic acid tert-butyl ester

Rendimiento 68.0%

Disolventes

dichloromethane

Condiciones de reacción

Tratamiento posterior

1. 1
   ConcentraciónConcentrate under reduced pressure
2. 2
   Lavadoeluting with a linear gradient from hexanes to ethyl acetate

Procedimiento

Add triethyl amine (0.025 mL) and acetic anhydride (0.013 mL) to a solution of 5-[2-amino-3-(3-fluoro-5-propoxy-phenyl)-1-hydroxy-propyl]-2-(3-fluoro-2-fluoromethyl-2-methyl-propoxy)-3-methyl-morpholine-4-carboxylic acid tert-butyl ester (67 mg) in dichloromethane (2 mL). Stir at room temperature for 2 hours. Concentrate under reduced pressure and subject to silica gel chromatography, eluting with a linear gradient from hexanes to ethyl acetate to afford 5-[2-acetylamino-3-(3-fluoro-5-propoxy-phenyl)-1-hydroxy-propyl]-2-(3-fluoro-2-fluoromethyl-2-methyl-propoxy)-3-methyl-morpholine-4-carboxylic acid tert-butyl ester (49 mg, 68%)

Fuente