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EXAMPLE 39 N-Z-N'-{N-(2S,3S)-trans-ethoxycarbonyloxirane-2-carbonyl]-o-fluoro-L-phenylalanyl}-1,4-diaminobutane In a mixture of dioxanes (10 ml) and water (5 ml), o-fluoro-L-phenylalanine (1.00 g, manufactured by Wako Pure Chemical Industries, Ltd.) was dissolved. To the solution were added, while stirring under ice-cooling conditions, a 1N aqueous solution of sodium hydroxide (5.46 ml) and di-tert-butyl dicarbonate (1.38 ml), followed by stirring for one hour at room temperature. The reaction mixture was concentrated, then the pH was adjusted to 2.5, followed by extraction with ethyl acetate (100 ml *3). The ethyl acetate layer was washed with water and a saturated saline, dried over anhydrous sodium sulfate. After concentration, the concentrate was crystallized from ethyl acetate--petroleum ether to yield N-Boc-o-fluoro-L-phenylalanine (1.32 g) as colorless crystals (yield 85%).
(R)-N-{(S)-2-(2-Fluoro-phenyl)-1-[(S)-4-guanidino-1-(thiazole-2-carbonyl)-butylcarbamoyl]-ethyl}-3-phenyl-2-phenylmethanesulfonylamino-propionamide[ No CAS ]
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