反应详情

To 2-cyanobenzene-1-sulfonyl chloride (201 mg, 1.00 mmol) in THF (10 mL), a 2M THF solution of ethylamine (5.0 mL, 10.0 mmol) was added. After stirring for 30 min, the reaction was concentrated then purified via preparative HPLC eluting with MeOH/H2O/TFA to provide 2-cyano-N-ethylbenzenesulfonamide (105 mg). The product was dissolved in MeOH (8 mL), conc. HCl (70 mg) was added, and the whole was hydrogenated at 30 psi for 3 h. The reaction was filtered and dried (Na2SO4) to provide 201A (123 mg, 49%). LC-MS: 215.1 (M+H)+.

1. concentrationthe reaction was concentrated
2. customthen purified via preparative HPLC
3. washeluting with MeOH/H2O/TFA