2-Chloro-6,7-dimethoxy-4-quinazolinamine → Benzyl (2S)-4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-2-[(2-methyl-2-propanyl)carbamoyl]-1-piperazinecarboxylate

Participants

Reaction Steps

A solution of 4-amino-2-chloro-6,7-dimethoxyquinazoline (0.78 g, 3.2535 mmol) and (S)-4-[(benzyloxy)carbonyl]-3-(1,1-dimethylethylamino) carbonyl piperazine (see Askin, D. et al., Tetrahedron Letters 1994, 35, 673-676) (1.04 g, 3.2535 mmol) in 2-propanol (6 mL) was heated at 90° C. (24 h). The solvent was removed in vacuo and the residue subjected to SGC (SiO2, 40 mm×240 mm, 0-10% MeOH/CH2Cl2) which afforded (S)-1-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-4-[(benzyloxy)carbonyl]-3-(1,1-dimethylethylamino)carbonyl piperazine.

Provenance & Evidence