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Synthesis 1997; 1997(12): 1446-1450
DOI: 10.1055/s-1997-1379
DOI: 10.1055/s-1997-1379
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Synthesis of an Ethyl 6-Amino-3,5-difluorosalicylate Derivative by Sequential Regioselective Directed ortho-Metalation; A Practical Synthesis of4',5-Diamino-3',6,8-trifluoroflavone, A Potent Antitumor Agent
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Publication History
Publication Date:
31 December 2000 (online)
The multigram scale synthesis of 4',5-diamino-3',6,8-trifluoroflavone, a potent antitumor agent, is described in which regioselective introduction of a carbonyl group into the ortho-position to the amide group of 2-[2,4-difluoro-5-(pivaloylamino)phenoxy]tetrahydropyran is achieved by using sequential direct ortho-metalations as the key step.
directed ortho-metalation - Stille coupling - flavone