Ethylenediamine → 5-chloro-thiophene-2-carboxylic acid ((3S,4S)-1-{[2-fluoro-4-(2-oxo-oxazolidin-3-yl)-phenylcarbamoyl]-methyl}-4-methoxy-pyrrolidin-3-yl)-amide

Participants

Reaction Steps

In analogy to example 25.3 {(3S,4S)-3-[(5-chloro-thiophene-2-carbonyl)-amino]-4-methoxy-pyrrolidin-1-yl}-acetic acid ethyl ester (example 25.2) was reacted with 3-(4-amino-3-fluoro-phenyl)-oxazolidin-2-one (prepared from 2-fluoro-4-iodoaniline and 2-oxazolidinone in the presence of Cu(I)I, ethylenediamine and potassium phosphate in dioxane at 110° C.) to give 5-chloro-thiophene-2-carboxylic acid ((3S,4S)-1-{[2-fluoro-4-(2-oxo-oxazolidin-3-yl)-phenylcarbamoyl]-methyl}-4-methoxy-pyrrolidin-3-yl)-amide as yellow solid. MS 497.5 ([M+H]+)

Provenance & Evidence