Ethanol → Ivabradine

Participants

Reaction Steps

In a 250-ml autoclave, 4 g of the product obtained in Example 1 and 2 g of Pd(OH)2 (20%, 50% moist) are added to a solution of ethanol (90 mL) and acetic acid (10 mL). After remaining in contact for 5 hours at ambient temperature under a hydrogen pressure of 5 bar, the reaction mixture is filtered over Celite®. The residue obtained after concentrating under reduced pressure is taken up in dichloromethane (100 mL) and then washed with saturated aqueous sodium bicarbonate solution. The oil obtained after drying the organic phase over MgSO4 and then concentrating under reduced pressure is purified by chromatography over silica (dichloromethane/ethanol/NH4OH 28%: 95/5/0.5), and 2.6 g of the title product are obtained in the form of an oil.

Provenance & Evidence