Dimethylformamide → HCID 59367666, compound

Participants

Reaction Conditions

Reaction Steps

4-{6-[(Naphthalen-2-ylmethyl)-amino]-3-aza-bicyclo[3.1.0]hex-3-yl}-benzoic acid trimethylsylanoate (1.29 mmol) was stirred in DMF (30 ml) at r.t. under N2. EDCl (297 mg, 1.55 mmol), HOBt (209 mg, 1.55 ml), intermediate D (89 μl, 6.45 mmol) and NEt3 (899 μl, 6.45 mmol) were added and the reaction stirred at 50° C. for 24 h. After this time the reaction was cooled to r.t. and diluted with water (100 ml). It was then extracted with DCM (2×100 ml), the organic layer dried (MgSO4) and concentrated in vacuo. The residue was purified by column chromatography (10% MeOH in DCM) to give the title compound as an orange oil (117 mg, 19%). LCMS purity 70%, m/z 474 [M+H]+.

Provenance & Evidence