[CH2:1]([N:3]([CH2:28][CH3:29])[C:4](=[O:27])[CH:5]([N:12]1[CH2:17][CH2:16][N:15]([C:18]2[CH:23]=[CH:22][C:21]([CH2:24]O)=[CH:20][C:19]=2[F:26])[CH2:14][CH2:13]1)[C:6]1[CH:11]=[CH:10][CH:9]=[CH:8][CH:7]=1)[CH3:2].C1(P(C2C=CC=CC=2)C2C=CC=CC=2)C=CC=CC=1.[C:49]1(=[O:59])[NH:53][C:52](=[O:54])[C:51]2=[CH:55][CH:56]=[CH:57][CH:58]=[C:50]12.N(C(OCC)=O)=NC(OCC)=O>C1COCC1>[O:54]=[C:52]1[C:51]2[C:50](=[CH:58][CH:57]=[CH:56][CH:55]=2)[C:49](=[O:59])[N:53]1[CH2:24][C:21]1[CH:22]=[CH:23][C:18]([N:15]2[CH2:14][CH2:13][N:12]([CH:5]([C:6]3[CH:11]=[CH:10][CH:9]=[CH:8][CH:7]=3)[C:4]([N:3]([CH2:28][CH3:29])[CH2:1][CH3:2])=[O:27])[CH2:17][CH2:16]2)=[C:19]([F:26])[CH:20]=1A solution of N,N-diethyl-2-[4-(2-fluoro-4-hydroxymethyl-phenyl)-piperazin-1-yl]-2-phenyl-acetamide (0.14 g, 0.362 mmol) in THF (3 mL) was added triphenylphosphine (96.5 mg), phthalimide (76.9 mg), and diethyl azodicarboxylate (50 μL), and the mixture stirred at rt. After 16 h, the solvent was removed and the residue purified on SiO2EtOAc/hexanes) to provide 115.5 mg of the title compound. MS (ESI): mass calcd. for C31H33FN4O3, 528.62. m/z found, 529.6 [M+H]+.
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