Diisopropylethylamine → HCID 70980685, compound

Participants

Reaction Steps

In a 25 mL round-bottomed flask was added (E)-3-(pyridin-3-yl)acrylic acid (38.0 mg, 0.255 mmol), N-(3-Dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride (48.9 mg, 0.255 mmol) and 1-Hydroxybenzotriazole hydrate (39.0 mg, 0.255 mmol) in Tetrahydrofuran (Volume: 4 ml) to give a light yellow suspension. Diisopropylethylamine (0.089 ml, 0.510 mmol) and (4-(8-oxa-3-azabicyclo[3.2.1]octan-3-ylsulfonyl)phenyl)methanamine (48 mg, 0.170 mmol; prepared according to example 5) were added sequentially and the suspension was allowed to stir at room temperature overnight before being filtered through Celite®. The cake was washed with THF then the combined filtrate was concentrated in vacuo and the resulting residue was purified by Preparative-HPLC to afford the product (68.0 mg).

Provenance & Evidence