4-Aminomethyl-tetrahydro-pyran-4-carboxylic acid methyl ester → 4-{[(1-Cyano-4-hydroxy-7-phenoxy-isoquinoline-3-carbonyl)-amino]-methyl}-tetrahydro-pyran-4-carboxylic acid methyl ester

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After a mixture of 1-cyano-4-hydroxy-7-phenoxy-isoquinoline-3-carboxylic acid methyl ester (151 mg), 4-aminomethyl-tetrahydro-pyran-4-carboxylic acid methyl ester (205 mg; commercially available) in MeOH (2 mL) was microwaved at 150° C. for 500 min; cooled, concentrated, the residue was partitioned between EtOAc and diluted HCl solution, EtOAc phase was washed with water and diluted NaCl solution, dried over anhydrous sodium sulfate, filtered, concentrated and column purified to give product (154 mg). LC MS ESI+: 462 (M+1)+.

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