Trifluoroacetic acid → HCID 59199262, compound

Participants

Reaction Steps

To a solution of the TFA salt of 4-(8-(piperidin-4-yloxy)quinazolin-2-ylamino)benzenesulfonamide in DCM was added isobutyraldehyde (2 eq) and a few drops of acetic acid. The mixture was stirred for 10 mins and to it was added sodiumtriacetoxyborohydride (1.5 eq) and the mixture was stirred for 1 h. The reductive amination went to completion, by LC/MS. The crude mixture was concentrated and purified on prep HPLC to give the product 4-(8-(1-isobutylpiperidine-4-yloxy)quinazolin-2-ylamino)benzenesulfonamide in 80% yield. ES/MS m/z 456.2 (MH+).

Provenance & Evidence