Journal
CHEMICAL & PHARMACEUTICAL BULLETIN
Volume 58, Issue 8, Pages 1107-1110Publisher
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.58.1107
Keywords
flavone; ipso-substitution; androgen; antagonist
Funding
- Ministry of Education, Culture. Sports, Science and Technology [20580115]
- fund for Agriomics project
- Uehara Memorial Foundation
- Grants-in-Aid for Scientific Research [20580115] Funding Source: KAKEN
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A variety of 5,4'-disubstituted flavones, which are anticipated to be androgen receptor antagonists to treat diseases mediated by the androgen receptor, were synthesized. It was found that an intramolecular ipso-substitution reaction via cesium enolate using 2-fluoro-6-hydroxyacetophenone and various benzoyl chlorides was effective in the preparation of 5-hydroxy-4'-alkylflavones.
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