Synthesis of 1,5-distributed-2-hydroxy-Gibbatetraen-6-ones

Synthesis of 1,5-distributed-2-hydroxy-Gibbatetraen-6-ones

1,5-disubstituted-2-hydroxy-gibbatetraen-6-ones are useful as estrogen receptor modulators and as precursors to estrogen receptor modulators. The current invention provides a method for the synthesis of 1,5-disubstituted-2-hydroxy-gibbatetraen-6-ones from simple indanone starting materials via a Rob...

Ausführliche Beschreibung

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Bibliographische Detailangaben
1. Verfasser: WILKENING ROBERT R.,FRIED AMY,PARKER DANNM L. JR
Format: Patent
Sprache:eng
Schlagworte:
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
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Beschreibung
Zusammenfassung:1,5-disubstituted-2-hydroxy-gibbatetraen-6-ones are useful as estrogen receptor modulators and as precursors to estrogen receptor modulators. The current invention provides a method for the synthesis of 1,5-disubstituted-2-hydroxy-gibbatetraen-6-ones from simple indanone starting materials via a Robinson-type annulation followed by an internal alkylation reaction. This invention further describes the novel use of a fluoroethyl substituent as a latent alkylating group for an internal cyclization reaction.