Cesium carbonate → 4-Chloro-2-[[2-chloro-4-(ethylsulfonyl)phenyl]amino]-benzenepropanoic acid

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Reaction Steps

A solution of the product from example 49 step (iii) (0.163 g) and the product of example 4 step (i) (0.200 g) and caesium carbonate (0.239 g) in NMP (10 ml) was refluxed at 100° C. for 3 hours. The mixture was partitioned between 2M sodium hydroxide and diethyl ether. The aqueous layer was acidified with 2M hydrochloric acid, extracted with ethyl acetate and the organic layer dried and concentrated under reduced pressure to give an oil. The residue was purified using RP prep HPLC. Yield 0.044 g.

Provenance & Evidence