Stereoselective synthesis of (-)-hydroxyclemastine as a versatile intermediate for the H1 receptor antagonist clemastine.
Hydroxyclemastine was targeted as a versatile analogue of clemastine with H1 receptor antagonist activity. Stereoselective synthesis of (-)-hydroxyclemastine was performed in which the key step was chelation-controlled diastereoselective 1,2-addition of Grignard reagent to alpha-alkoxyketone.
Jung
Jung Wha
JW
College of Pharmacy, Sookmyung Women's University, Seoul 140-742, Korea.
Kim
Hee-Doo
HD
D002974:Clemastine / Q000138:chemical synthesis*; D006634:Histamine H1 Antagonists / Q000138:chemical synthesis*; D013237:Stereoisomerism
D006634:Histamine H1 Antagonists; D002974:Clemastine