4-aminotetrahydro-2H-pyran-4-carboxylic acid → 4-[({4-[(3-chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl}methyl)amino]tetrahydro-2H-pyran-4-carboxylic acid

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Reaction Steps

4-(3-Chloro-2-fluoroanilino)-7-methoxyquinazoline-6-carbaldehyde was coupled with 4-aminotetrahydro-2H-pyran-4-carboxylic acid using an analogous method to that described for the equivalent step in Example 1 to give 4-[({4-[(3-chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl}methyl)amino]tetrahydro-2H-pyran-4-carboxylic acid; 1H NMR Spectrum: (DMSO-d6) 1.62-1.74 (m, 2H), 1.92-2.03 (m, 2H), 3.46-3.56 (m, 2H), 3.76 (s, 2H), 3.76-3.85 (m, 2H), 3.94 (s, 3H), 7.18 (s, 1H), 7.23-7.31 (m, 1H), 7.43-7.57 (m, 2H), 8.38 (s, 1H), 8.42 (s, 1H), 9.81 (brs, 1H). Mass Spectrum: (M+H)+ 461.

Provenance & Evidence