4-Amino-1-(tert-butoxycarbonyl)piperidine-4-carboxylic acid → 1-(Tert-butoxycarbonyl)-4-[({4-[(3-chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl}methyl)amino]piperidine-4-carboxylic acid

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Reaction Steps

4-(3-Chloro-2-fluoroanilino)-7-methoxyquinazoline-6-carbaldehyde was coupled with 4-amino-1-(tert-butoxycarbonyl)piperidine-4-carboxylic acid using an analogous method to that described for the equivalent step in Example 1 to give 1-(tert-butoxycarbonyl)-4-[({4-[(3-chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl}methyl)amino]piperidine-4-carboxylic acid; 1H NMR Spectrum: (DMSO d6) 1.39 (s, 9H); 1.70 (m, 2H); 1.86 (m, 2H); 3.43 (m, 4H); 3.76 (s, 2H); 3.96 (s, 3H); 7.19 (s, 1H); 7.28 (t, 1H); 7.48 (t, 1H); 7.55 (t, 1H); 8.37 (s, 1H); 8.43 (s, 1H); 9.78 (s, 1H); Mass Spectrum: (M+H)+ 560.

Provenance & Evidence