Trifluoroacetic acid → N-benzyl-N-[(3-chloropropyl)sulfonyl]-3-cyclohexyl-1-(2-{methyl[2-(methylamino)ethyl]amino}-2-oxoethyl)-2-phenyl-1H-indole-6-carboxamide hydrochloride

Participants

Reaction Steps

A solution of the crude tert-butyl {2-[{[6-({benzyl[(3-chloropropyl)sulfonyl]amino}carbonyl)-3-cyclohexyl-2-phenyl-1H-indol-1-yl]acetyl}(methyl)amino]ethyl}methylcarbamate in DCM) (0.09 M) was treated with TFA (140 eq) at 0° C. The reaction was allowed to reach RT in about 1 h. The solvent was then removed in vacuo, a 2 M solution HCl in Et2O was added and the volatiles removed in vacuo. Acetonitrile was added and the precipitate was collected by filtration to afford clean compound (30%). (ES+) m/z 677 (M+H)+

Provenance & Evidence