Cesium acetate → Erlotinib Acetate

Participants

Reaction Steps

The title product of Example 34 (160 mg, 0.368 mmol); was treated with cesium acetate (707 mg, 3.68 mmol) in DMF (3 mL) at 120° C. under an atmosphere of N2 for 16 hours. The reaction mixture was partitioned between brine and CHCl3, and the organic extract was washed with brine, dried over Na2SO4, filtered and concentrated in vacuo to afford a residue (288 mg) which was recrystallized from ethyl acetate/hexanes. (134 mg; M.P.134°-135° C.; LC-MS: 422 (MH+); anal. RP18-HPLC RT: 4.43 min.).

Provenance & Evidence