Reacción #577254

Ecuación de reacción

(R)-4-(di-tert-butoxy-phosphoryloxymethyl)-4-(2-{4-[2-(3-fluoro-phenoxy)-ethoxy]-phenyl}-ethyl)-2,2-dimethyl-oxazolidine-3-carboxylic acid tert-butyl ester

→

phosphoric acid mono-((R)-2-amino-4-{4-[2-(3-fluoro-phenoxy)-ethoxy]-phenyl}-2-hydroxymethyl-butyl)ester

Disolventes

HCl

Condiciones de reacción

Tratamiento posterior

1. 1
   Temperaturais then heated to 95° C. for 2 hours
2. 2
   Concentraciónconcentrated to dryness
3. 3
   workup.DISSOLUTIONThe residue is re-dissolved in ethyl acetate
4. 4
   Otroprecipitated with hexanes
5. 5
   FiltraciónThe solid is filtered off
6. 6
   Lavadowashed with dry ether
7. 7
   Otrodried in vacuo

Procedimiento

Finally, a solution of (R)-4-(di-tert-butoxy-phosphoryloxymethyl)-4-(2-{4-[2-(3-fluoro-phenoxy)-ethoxy]-phenyl}-ethyl)-2,2-dimethyl-oxazolidine-3-carboxylic acid tert-butyl ester (70 mg, 0.10 mmol) in conc. HCl (2 ml). is stirred at room temperature for one hour and is then heated to 95° C. for 2 hours, then concentrated to dryness. The residue is re-dissolved in ethyl acetate and precipitated with hexanes. The solid is filtered off, washed with dry ether and dried in vacuo to afford phosphoric acid mono-((R)-2-amino-4-{4-[2-(3-fluoro-phenoxy)-ethoxy]-phenyl}-2-hydroxymethyl-butyl)ester as a colorless powder.

Fuente