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Stereoselective synthesis of (-)-hydroxyclemastine as a versatile intermediate for the H-1 receptor antagonist clemastine
- Authors
- Jung, Jung Wha; Kim, 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
- Pages
- 5
- Journal Title
- ARCHIVES OF PHARMACAL RESEARCH
- Volume
- 30
- Number
- 12
- Start Page
- 1521
- End Page
- 1525
- ISSN
- 0253-6269
1976-3786
- 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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