反应详情

4-[(3-chloro-2-fluorophenyl)amino]-7-methoxyquinazoline-6-carbaldehyde was coupled with 3-amino-1-(tert-butoxycarbonyl)pyrrolidine-3-carboxylic acid (commercially available or may be prepared made using analogous methodology as that described for the preparation of 4-amino-1-(tert-butoxycarbonyl)piperidine-4-carboxylic acid in J. Org. Chem. 1996, 61, 7650-7651). The resultant product was deprotected and methylated by reaction with aqueous formaldehyde using analogous methods to those described for the equivalent steps in Example 68 to give 3-[({4-[(3-chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl}methyl)(methyl)amino]-1-methylpyrrolidine-3-carboxylic acid as a pale yellow foam; Mass Spectrum: (M+H)+ 474.

1. custommay be prepared