4-Methylmorpholine → HCID 21968056, compound

Participants

Reaction Steps

Dissolve the title compound from Example 2 (1 mmol) in anhydrous N,N-dimethylformamide (DMF, 10 mL) and add 1-hydroxybenzotriazole hydrate (1 mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (1 mmol), ammonium chloride (1 mmol) and N-methylmorpholine (1 mmol). Stir the resulting mixture at room temperature under nitrogen overnight. Concentrate in vacuo to provide a residue and dilute with dichloromethane, wash with 1M hydrochloric acid and brine, then dry over anhydrous magnesium sulfate. Filter and concentrate in vacuo to afford (+)-4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(R)-yl)-1-[[4-cyano-1-(methylsulfonyl)-4-pyridinyl]acetyl]piperidine.

Provenance & Evidence