HCID 56967177, compound → HCID 67512675, compound

Participants

Reaction Steps

1.15 g of 4-cyano-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}-benzenesulfonamide in 5 ml of THF and 12 ml of methanolic ammonia solution (10%) are hydrogenated in a suitable pressure apparatus in the presence of 1.00 g of sponge nickel catalyst (Johnson-Matthey) at 50° C. and 5 bar for 17 hours. The catalyst is filtered off, rinsed with copious MeOH and THF, and the entire filtrate is evaporated, giving 819 mg of 4-aminomethyl-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}-benzenesulfonamide having a content of 82.4% (yield 59.4%); MS-FAB (M+H+)=540.2; Rf (polar method): 1.75 min.

Provenance & Evidence