Biphenyl-3-ylcarbamic acid phenyl ester → (S)-4-[4-((S)-4-Hydroxy-6-aza-spiro[2.5]oct-6-yl)-butyl]-2-methyl-3-oxo-piperazine-1-carboxylic acid biphenyl-3-ylamide

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A solution of (S)-1-[4-((S)-4-hydroxy-6-aza-spiro[2.5]oct-6-yl)-butyl]-3-methyl-piperazin-2-one (intermediate 27; 50 mg, 0.17 mmol) and biphenyl-3-ylcarbamic acid phenyl ester (PCT Int. Appl. WO20050443810; 49 mg, 0.17 mmol) in acetonitrile (1 mL) was stirred at room temperature for 72 h, then concentrated under vacuum. Chromatography (SiO2; dichloro-methane/methanol/25% aq. ammonia solution 90:10:0.25) furnished the title compound (69 mg, 83%). White foam, MS (ISP)=491.3 (M+H)+.

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