Hydrogen Peroxide → HCID 89647760, compound

Participants

Reaction Conditions

Reaction Steps

To a stirred solution of N—[(S)-2-(8-Cyano-quinazolin-5-ylamino)-2-(3-fluoro-phenyl)-ethyl]-N-methyl-4-nitro-benzenesulfonamide (120.00 mg; 0.24 mmol; 1.00 eq.) in DMSO (8 ml) was added aqueous 2.0M NaOH (0.59 ml; 1.18 mmol; 5.00 eq.) and aqueous 35% hydrogen peroxide (0.14 ml; 1.42 mmol; 6.00 eq.) and continued stirring at 40° C. overnight. The crude product was purified by prep-HPLC to yield the desired product, which was then added of acetonitrile (2 ml), thiophenol (0.1 ml), CsCO3 (200 mg), and stirred at 40° C. overnight. The crude was purified by prepHPLC to afford the title product. LC-MS (M+H=434, obsd.=434).

Provenance & Evidence