Reacción #10298

Ecuación de reacción

potassium formate

4-{4-[5-(4-methanesulfonyl-phenyl)-4-methyl-2-oxo-oxazolidin-3-yl]-butyl}-5-oxo-[1,4]diazepane-1-carboxylic acid tert-butyl ester

isopropanol

→

4-{4-[2-(4-methanesulfonyl-phenyl)-1-methyl-ethylamino]-butyl}-5-oxo-[1,4]diazepane-1-carboxylic acid tert-butyl ester

Rendimiento 97.8%

Disolventes

water

water

Condiciones de reacción

Tratamiento posterior

1. 1
   Temperaturaheated to 50°–60° C
2. 2
   workup.STIRRINGThe mixture was stirred for 3 hours
3. 3
   Temperaturawas then cooled
4. 4
   Filtraciónfiltered

Procedimiento

A mixture of 10 g 4-{4-[5-(4-methanesulfonyl-phenyl)-4-methyl-2-oxo-oxazolidin-3-yl]-butyl}-5-oxo-[1,4]diazepane-1-carboxylic acid tert-butyl ester, 1 g of 20% palladium hydroxide on carbon, 10 ml water, and 90 ml isopropanol was stirred and heated to 50°–60° C. A solution of 3.5 g potassium formate in 5 ml water was slowly added. The mixture was stirred for 3 hours and was then cooled and filtered. The filtrate was stripped to yield ca. 9 g of 4-{4-[2-(4-methanesulfonyl-phenyl)-1-methyl-ethylamino]-butyl}-5-oxo-[1,4]diazepane-1-carboxylic acid tert-butyl ester.

Fuente