PDF herunterladen
Synthesis 1997; 1997(12): 1446-1450
DOI: 10.1055/s-1997-1379
paper
© Georg Thieme Verlag, Rüdigerstr. 14, 70469 Stuttgart, Germany. All rights reserved. This journal, including all individual contributions and illustrations published therein, is legally protected by copyright for the duration of the copyright period. Any use, exploitation or commercialization outside the narrow limits set by copyright legislation, without the publisher's consent, is illegal and liable to criminal prosecution. This applies in particular to photostat reproduction, copying, cyclostyling, mimeographing or duplication of any kind, translating, preparation of microfilms, and electronic data processing and storage.

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

Tsutomu Akama1 , Kimihisa Ueno, Hiromitsu Saito, Masaji Kasai2
  • 1Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Co. Ltd., 1188 Shimotogari, Nagaizumi-cho, Shizuoka 411, Japan, Fax +81(427)268330; E-mail: tsutomu.akama@kyowa.co.jp
  • 2Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Co. Ltd., 1188 Shimotogari, Nagaizumi-cho, Shizuoka 411, Japan, Fax +81(427)268330
Weitere Informationen

Publikationsverlauf

Publikationsdatum:
31. Dezember 2000 (online)

  als PDF herunterladen  Lizenzen und Reprints Alle Artikel dieser Rubrik

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