摘要：

The syntheses of tritium labeled ( S )-3-(5-chloro-2-[OC 3 H 3 ]methoxyphenyl-1,3-dihydro-3-fluoro-6-(trifluoromethyl)-1H-indol-2-one, and carbon-14 ( S )-3-(5-chloro-2-methoxyphenyl)-1,3-dihydro-3-fluoro-6-(trifluoromethyl)-2H-[2,3- 14 C 2 ] indol-2-one are reported. The 3 H-labeled compound was prepared in a two-step synthesis from C 3 H 3 I. The final product was purified via chiral HPLC to yield the desired enantiomer in a 4% radiochemical yield and a specific activity of 60 Ci/mmol. The 14 C-labeled compound was prepared in a four-step synthesis from diethyl [carboxylate- 14 C 1 , 2 ] oxalate. The final product was purified via chiral HPLC to yield the desired enantiomer in a 20% radiochemical yield and a specific activity of 28.4 μCi/mg. Copyright 2002 John Wiley & Sons, Ltd.

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