tert-Butyl isocyanate → 4-({[(tert-Butylamino)carbonyl]amino}methyl)-2-(4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}piperidin-1-yl)-1,3-thiazole-5-carboxylic acid

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Reaction Steps

Ethyl 4-(aminomethyl)-2-(4-{[(3,4-dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}piperidin-1-yl)-1,3-thiazole-5-carboxylate (Example 246; 200 mg; 0.424 mmol) was dissolved in DCM (4 ml). tert-Butyl isocyanate (130 mg; 1.28 mmol) was added and the mixture stirred at room temperature for 1 h. The solvent was removed in vacuo and the ester (215 mg), LCMS:561 was treated with LiOH/THF in a manner analogous to Example 31 to give the title compound (290 mg).

Provenance & Evidence