Formic Acid → HCID 53329715, compound

Participants

Reaction Steps

A solution of (2-(2-amino-3-morpholinoquinolin-6-yl)-3-(3,3-dimethylbut-1-ynyl)phenyl)(pyrrolidin-1-yl)methanone (188 mg, 0.390 mmol, see Example 45) in formic acid (>96%) (10 mL, 265 mmol) was heated to 110° C. After 4 days CH2Cl2 was added and the solution was washed with water and sodium carbonate solution. The organic phase was separated and dried over MgSO4. The solvent was removed under reduced pressure and the remaining residue was purified by preparative HPLC (10-100% water with 0.1% TFA/CH3CN, 11 min). The obtained product was eluted on an SCX cartridge with MeOH followed by 2M NH3/MeOH. The basic fraction was concentrated to afford the titled compound as a white powder. MS (ESI, pos. ion) m/z: 501 (M+1).

Provenance & Evidence