Preparation and Use of Tritiated Schwartz' Reagent (ZrCp₂Cl³H)

E. M. Zippi National Tritium Labeling Facility, Structural Biology Division, Lawrence Berkeley Laboratory, Berkeley, CA, 94720, U.S.A.; Sandoz Pharma Ltd, Chemical Research and Development, Basle, CH-4002, Switzerland

H. Andres Sandoz Pharma Ltd, Chemical Research and Development, Basle, CH-4002, Switzerland

H. Morimoto National Tritium Labeling Facility, Structural Biology Division, Lawrence Berkeley Laboratory, Berkeley, CA, 94720, U.S.A.

P. G. Williams National Tritium Labeling Facility, Structural Biology Division, Lawrence Berkeley Laboratory, Berkeley, CA, 94720, U.S.A.

Abstract

Treatment of Li³H with ZrCp₂Cl₂ in THF affords ZrCp₂Cl³H. By the action of ZrCp₂Cl³H on an acetylene, it is possible to stereo- and regioselectively introduce tritium into the vinylic position, a site which has often proved to be metabolically stable in complex molecules. In addition, ZrCp₂Cl³H may be used to regioselectively label olefins with tritium.

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Preparation and Use of Tritiated Schwartz' Reagent (ZrCp₂Cl³H)

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Preparation and Use of Tritiated Schwartz' Reagent (ZrCp₂Cl³H)