Diisopropylethylamine → (R)-1-(4-Fluorophenyl)-6-[6-((R)-3-fluoropyrrolidin-1-yl)-pyridine-3-sulfonyl]-4a-methoxymethyl-4,4a,5,6,7,8-hexahydro-1H-1,2,6-triaza-cyclopenta[b]naphthalene

Participants

Reaction Steps

A solution of (R)-6-(6-chloropyridine-3-sulfonyl)-4a-methoxymethyl-1-(4-fluorophenyl)-4,4a,5,6,7,8-hexahydro-1H-1,2,6-triazacyclopenta[b]naphthalene (0.098 g), diisopropylethylamine (0.194 g) and (R)-3-fluoropyrrolidine hydrochloride in acetonitrile was heated at 130° C. in a microwave reactor for 45 minutes. The solution was diluted with ethyl acetate, washed with water followed by brine, dried over sodium sulfate, filtered and the filtrate concentrated under reduced pressure. The residue was purified by column chromatography on silica gel, eluting with ethyl acetate in cyclohexane (0 to 3:2 by volume), to afford the title compound as a white solid (0.089 g). LCMS (Method F): 542 (M+H)+, Retention time 5.0 minutes

Provenance & Evidence