Sodium Iodide → HCID 67032496, compound

Participants

Reaction Steps

A mixture of 3-[2-(4-hydroxy-phenyl)-morpholin-4-yl]-propionic acid tert-butyl ester) (76.8 mg; 0.25 mmol), Cs2CO3 (241 mg; 0.74 mmol), and NaI (3.7 mg, 25 μmol) in CH3CN/THF (6:4; 2.5 mL) was stirred for three hours at RT. Subsequently, benzyl chloride (35 μL; 0.3 mmol) in CH3CN (1 mL) was added and the resulting mixture was heated at 60° C., for 20 h. After cooling to RT the solvents were removed in vacuo. The residue was partitioned between CH2Cl2 and 1M aqueous K2CO3. The layers were separated and the aqueous layer washed with CH2Cl2. The combined organic layers were concentrated in vacuo, and the residue dried under vacuum, at 40° C., overnight. The obtained product was used as such in the next step.

Provenance & Evidence