Synthesis of 3H and 14C labeled (S)‐3‐(5‐chloro‐2‐methoxyphenyl)‐1,3‐dihydro‐3‐fluoro‐6‐(trifluoromethyl)‐2H‐indol‐2‐one, maxipost. An agent for post‐stroke neuroprotection
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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DOI:
10.1002/jlcr.652
被引量:
年份:
2003
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