Concise Synthesis of (2S,3R)-3-Hydroxy-2-phenylpiperidine: An Advanced Key Intermediate of Human Non-Peptide NK-1 Receptor Antagonists

[摘要]：The rapid, high-yielding synthesis of (2S,3R)-3-hydroxy-2-phenylpiperidine, a known advanced key intermediate of some non-peptide human NK-1 receptor antagonists such as (+)-CP-99,994, (+)-CP-122,721 and (+)-LP-733,060, is reported. This synthesis involves the stereoselective addition of racemic 3-(methoxymethoxy)allenylzinc bromide to enantiopure (R-S,E)-N-2-benzylidene-2-methylpropane-2-sulfinamide and a ring-closing metathesis reaction as the key steps. Following this procedure, (2S,3R)-3-hydroxy-2-phenylpiperidine is obtained in seven steps ill 56.2% overall yield.

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