Abstract
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 α-alkoxyketone.
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Jung, J.W., Kim, HD. Stereoselective synthesis of (-)-hydroxyclemastine as a versatile intermediate for the h1 receptor antagonist clemastine. Arch Pharm Res 30, 1521–1525 (2007). https://doi.org/10.1007/BF02977320
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DOI: https://doi.org/10.1007/BF02977320