The synthesis of [14C]‐ and [2H]‐labeled LY253351 (YM12617–1), a potent α1‐receptor antagonist, which is potentially useful in the treatment of benign prostatic hypertrophy (BPH) is described. The [14C]‐isotopomer was synthesized from [14C]‐potassium cyanide in nine steps in 1.5% radiochemical yield. One of the key intermediates, [14C]‐4‐methoxyphenylacetone, was synthesized from [14C]‐4‐methoxyphenylacetyl chloride by a Pd(0)‐catalyzed reaction with tetramethylstannane. The [2H]‐labeled material was synthesized by a Pd/C catalyzed reductive amination with deuterium gas.
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