Nitric Acid → Arasertaconazole mononitrate

Participants

Reaction Steps

880 mg (2.01 mmol) of (R)-(−)-1-[2-(7-chlorobenzo[b]thiophen-3-yl-methoxy)-2-(2,4-dichlorophenyl)-ethyl]-1H-imidazole are dissolved in 5 ml of 96% ethanol. 1 ml of water is added and heated at a temperature between 35 and 37° C. To the obtained solution, 0.23 ml of 60% nitric acid (3 mmol, 1.5 eq.) are added. Then 3 ml of water are added and cooled first at room temperature and thereafter at 10° C. for 1 hour. The formed solid is filtered, washed twice with 4 ml of water and dried at vacuum for 24 hours to give 0.9 g (R=89%) of (R)-(−)-1-[2-(7-chlorobenzo[b]thiophen-3-yl-methoxy)-2-(2,4-dichlorophenyl)-ethyl]-1H-imidazole mononitrate.

Provenance & Evidence