Water → Trifluoroacetic acid

Participants

Reaction Steps

To solution of crude 3-[3-(N,N-diethyl-carbamimidoyl)-9H-xanthen-9-yl]-8-aza-bicyclo[3.2.1]octane-8-carboxylic acid tert-butyl ester, 3m (0.34 g) in dichloroethane (2 mL) was added H2O (0.1 mL) and TFA (2 mL). The mixture was stirred at rt for 1 h and evaporated. The residue was purified via reverse phase HPLC (eluent: CH3CN in water containing 0.1% TFA), yielding 0.263 g (56%) for two steps) of 9-(8-aza-bicyclo[3.2.1]oct-3-yl)-N,N-diethyl-9H-xanthene-3-carboxamidine, 4m as a TFA salt (MS m/z (MH+) 390.3.

Provenance & Evidence