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KMID : 0043320070300121521
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Archives of Pharmacal Research
2007 Volume.30 No. 12 p.1521 ~ p.1525
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Stereoselective Synthesis of (-)-Hydroxyclemastine as a Versatile Intermediate for the H1 Receptor Antagonist Clemastine
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Jung Jung-Wha
Kim Hee-Doo
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Abstract
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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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KEYWORD
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Hydroxyclemastine, Clemastine, H1 receptor antagonist, Chelation, Stereoselective
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