An Effective Synthesis of 5,4 '-Disubstituted Flavones via a Cesium Enolate Assisted Intramolecular ipso-Substitution Reaction

作者：Matsugi Masato^*; Takeda Masaki; Takahashi Ayano; Tazaki Takahide; Tamura Hiroto; Shioiri Takayuki

来源：Chemical & Pharmaceutical Bulletin, 2010, 58(8): 1107-1110.

• flavone
• ipso-substitution
• androgen
• antagonist

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.

• 出版日期2010-8