Trifluoroacetic acid → [2-((S)-1-Aminoethyl)-3-cyclopropyl-5-fluoro-3H-benzoimidazol-4-yl]-morpholin-4-yl-methanone

Participants

Reaction Steps

TFA (1 mL) was added to a stirring solution of {(S)-1-[1-cyclopropyl-6-fluoro-7-(morpholine-4-carbonyl)-1H-benzoimidazol-2-yl]ethyl}carbamic acid tert-butyl ester (380 mg, 0.88 mmol) in DCM (3 mL). After stirring at RT for 2 h, the reaction mixture was diluted with MeOH and loaded onto an Isolute® SCX-2 cartridge. The cartridge was washed with MeOH followed by 2M NH3/MeOH. The basic fractions were combined and concentrated in vacuo to afford the title compound as a pale yellow oil (214 mg, 73%). LCMS (Method B): RT 1.62 and 1.70 min [M+H]+ 333.12

Provenance & Evidence