Triphenylphosphine → HCID 59199319, compound

Participants

Reaction Steps

To a solution of triphenylphosphine (2 eq) in THF was added di-terbutylazodicarboxylate (2 eq). The mixture was stirred 15 minutes at ambient temperature under nitrogen atmosphere. To that was added 1-isopropylpiperidine-4-ol (5 eq). The mixture was stirred 15 minutes at ambient temperature followed by addition of 2-(4-fluoro-3-methylphenylamino) quinazolin-7-ol (1 eq). The mixture was stirred overnight at ambient temperature. The LC-MS of reaction mixture shows the presence of two product (2:1) with identical mass. The reaction mixture was concentrated and purified by semi-preparative HPLC to provide (N-(4-fluoro-3-methylphenyl)-7-(1-isopropyl-piperidin-4-yloxy)-quinazolin-2-amine as a major product ES/MS m/z 395.2 (MH+).

Provenance & Evidence