With the main objective of examining the pharmacokinetics of flutamide, flutamide-d(7) and its main metabolite-d(6) have been prepared. By carboxylation of Grignard-derivative (IV), deuterocarboxylic acid (V) was prepared from which acyl chloride (VI) was obtained by reaction with (COCl)(2). Subsequent reaction of (VI) with 4-nitro-3-trifluoromethylaniline afforded (I). Compound (X) was obtained starting from hydroxyacid (IX), through reaction with TMSCI, (COCl)(2) and subsequent condensation with 4-nitro-3-trifluoromethylaniline. Desilylation of(X) by tetrabutylammonium fluoride, gave (II).
Synthesis of flutamide-d(7) and its main metabolite-d(6) / D. Passarella, M. Martinelli, C. Passarotti, M. Valenti. - In: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS. - ISSN 0362-4803. - 42:3(1999), pp. 275-279.
Synthesis of flutamide-d(7) and its main metabolite-d(6)
D. PassarellaPrimo
;
1999
Abstract
With the main objective of examining the pharmacokinetics of flutamide, flutamide-d(7) and its main metabolite-d(6) have been prepared. By carboxylation of Grignard-derivative (IV), deuterocarboxylic acid (V) was prepared from which acyl chloride (VI) was obtained by reaction with (COCl)(2). Subsequent reaction of (VI) with 4-nitro-3-trifluoromethylaniline afforded (I). Compound (X) was obtained starting from hydroxyacid (IX), through reaction with TMSCI, (COCl)(2) and subsequent condensation with 4-nitro-3-trifluoromethylaniline. Desilylation of(X) by tetrabutylammonium fluoride, gave (II).Pubblicazioni consigliate
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