反应详情

2-[5-Benzyloxycarbonylamino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1(S)-benzyl-3,3-difluoro-2(R)-hydroxy-3-[N-(benzyl)caramoyl]propyl]acetamide was synthesized in the same manner as in Example 1. That is, 2-[5-benzyloxycarbonylamino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]acetic acid (title compound in Reference Example 3, mixture with benzyl alcohol, 380 mg, 0.897 mmol) was treated with N-[4(S)-amino-2,2-difluoro-3(R)-hydroxy-5-phenylpentanoyl]benzylamine (title compound in Reference Example 6: 300 mg, 0.897 mmol), HOBT (242 mg, 1.79 mmol) and WSCI hydrochloride (206 mg, 1.08 mmol) in dichloromethane (30 mL) to give 590 mg (92%) of the target compound as colorless crystals.

1. custom2-[5-Benzyloxycarbonylamino-2-(4-fluorophenyl)-6-oxo-1,6-dihydro-1-pyrimidinyl]-N-[1(S)-benzyl-3,3-difluoro-2(R)-hydroxy-3-[N-(benzyl)caramoyl]propyl]acetamide was synthesized in the same manner as in Example 1