Dichloromethane → Tert-butyl 4-(2-(3-chloro-4-morpholinophenylamino)-5-methylquinazolin-8-yloxy)piperidine-1-carboxylate

Participants

Reaction Steps

To a solution of tert-butyl 4-(5-bromo-2-(3-chloro-4-morpholinophenylamino) quinazolin-8-yloxy)piperidine-1-carboxylate (See example 45 for synthesis) (1 eq) in DMF was added 2M sodium carbonate solution, trimethylboroxine (3 eq) and Pd (dppf)2Cl2.CH2Cl2 (0.05 eq). The reaction mixture was micro waved for 10 min at 120° C. The reaction mixture was then partitioned between ethyl acetate and water. The organic layer was washed with brine, dried, concentrated and purified by semi-preparative HPLC to provide pure product. ES/MS m/z 554.1 (MH+).

Provenance & Evidence