Chiral aziridine ring opening: facile synthesis of (R)-mexiletine and (R)-phenoxybenzamine hydrochloride

Abstract A simple and efficient synthesis of chiral drugs ( R )-mexiletine 1 , an anti-arrhythmic drug and ( R )-phenoxybenzamine hydrochloride 2 , an anti-hypertensive drug has been described via controlled reductive ring opening of chiral aziridine as a key step. The target compounds 1 and 2 were obtained in overall yields of 34% and 10.5%, respectively.