(Development of radionuclides from the LAMPF facility)

TL;DRAbstract

The research objectives and goals of 1983--84 to date include further investigation of 1-halogenated and B-/C-ring halogenated and radio halogenated estradiol derivatives for potential use as receptor-binding radiopharmaceuticals. Our group has devised synthetic routes to 1-bromo, 1-chloro- and 1-fluoroestradiol via electrophilic halogenation of the aromatic A-ring. Work is presently underway to prepare the 1-iodo derivative using a similar methodology. The 11 {beta}-methoxy, 17 {alpha}-ethynyl and 11 {beta}-methoxy-17 {alpha}-ethynyl derivatives are of synthetic interest if the in vitro binding affinities of the parent compounds are favorable. The B- and C-ring vinyl halides' which were proposed in the current contract could not be prepared using the hydrazone intermediates described. Presently, other methods which show promise are being investigated. Stable B-ring brominated derivatives of estradiol have been prepared by our group. Their in vitro properties are currently under invest

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