Synthesis of carbon??14 labeled Taxol®(paclitaxel)

…, JE Swigor, J Kant, DR Schroeder

Index: Walker; Swigor; Kant; Schroeder Journal of Labelled Compounds and Radiopharmaceuticals, 1994 , vol. 34, # 10 p. 973 - 980

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Abstract

Abstract Reductive cleavage of the C13 side chain of Taxol®(1, paclitaxel) followed by regioselective silylation gave 7-triethylsilylbaccatin III (4). 3-O-Triethylsilylation of 5 and subsequent reaction with benzoyl chloride-C7-14 C gave azetidinone 7. Coupling of 4 and 7 followed by deprotection gave 1.26 g of Taxol®-N3′-14 C (11) having a specific activity of 26.5 mCi/mmol and a radiochemical purity of 95%.

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