Ethyl (R)-2-(trifluoromethylsulfonyloxy)propionate → n-({4-[(3-Chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl}methyl)-n-ethyl-l-alanine

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Reaction Steps

N-(3-Chloro-2-fluorophenyl)-6-[(ethylamino)methyl]-7-methoxyquinazolin-4-amine was coupled with ethyl O-trifluoromethanesulfonyl-D-lactate and hydrolysed using analogous methods to those described for the equivalent steps in Example 46 to give N-({4-[(3-chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl}methyl)-N-ethyl-L-alanine; 1H NMR Spectrum: (DMSO-d6) 1.03 (t, 3H); 1.29 (d, 3H); 2.71 (q, 2H); 3.56 (q, 1H); 3.86 (d, 1H); 3.94 (m, 4H); 7.19 (s, 1H); 7.28 (t, 1H); 7.48 (m, 1H); 7.56 (m, 1H); 8.41 (m, 2H); 9.76 (brs, 1H); Mass Spectrum: (M+H)+ 433.

Provenance & Evidence