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Stereoselective synthesis of (-)-hydroxyclemastine as a versatile intermediate for the H-1 receptor antagonist clemastine

Authors
Jung, Jung WhaKim, Hee-Doo
Issue Date
Dec-2007
Publisher
PHARMACEUTICAL SOC KOREA
Keywords
hydroxyclemastine; clemastine; H-1 receptor antagonist; chelation; stereoselective
Citation
ARCHIVES OF PHARMACAL RESEARCH, v.30, no.12, pp.1521 - 1525
Journal Title
ARCHIVES OF PHARMACAL RESEARCH
Volume
30
Number
12
Start Page
1521
End Page
1525
URI
https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/14609
DOI
10.1007/BF02977320
ISSN
0253-6269
Abstract
Hydroxyclemastine was targeted as a versatile analogue of clemastine with H-1 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.
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