Ethanol → Cyclopropanesulphonic acid 3'-amino-4-(2,4-diamino-pyrimidin-5-ylmethyl)-6-ethoxy-5'-fluoro-biphenyl-2-yl ester

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Reaction Steps

Starting from cyclopropanesulphonic acid 5-(2,4-diamino-pyrimidin-5-ylmethyl)-3-ethoxy-2-iodo-phenyl ester (294 mg; 0.60 mmol) and N-(5-iodo-3-fluoro-phenyl)-2,2,2-trifluoroacetamide (preparation described in example 4t) (333 mg; 1.0 mmol) (first step in 12 ml dioxane instead of dimethylformarmide with bis-triphenylphosphine-palladium dichloride (56 mg; 0.08 mmol) and second step in dimethoxyethane (8 ml) and ethanol (2 ml) with tetrakis-triphenylphosphine-palladium (69 mg; 0.06 mmol)), 147 mg (30%) cyclopropanesulphonic acid 3′-amino-4-(2,4-diamino-pyrimidin-5-ylmethyl)-6-ethoxy-5′-fluoro-biphenyl-2-yl ester are obtained as a colourless powder.

Provenance & Evidence