[C:1]1([CH2:7][CH2:8][NH2:9])[CH:6]=[CH:5][CH:4]=[CH:3][CH:2]=1.[F:10][C:11]1[CH:18]=[CH:17][CH:16]=[CH:15][C:12]=1[CH:13]=O.[SH:19][CH:20]([CH2:24][C:25]([OH:27])=[O:26])[C:21](O)=[O:22].C(OC)(OC)OC>CCOC(C)=O>[F:10][C:11]1[CH:18]=[CH:17][CH:16]=[CH:15][C:12]=1[CH:13]1[N:9]([CH2:8][CH2:7][C:1]2[CH:6]=[CH:5][CH:4]=[CH:3][CH:2]=2)[C:21](=[O:22])[CH:20]([CH2:24][C:25]([OH:27])=[O:26])[S:19]1A solution of phenylethylamine (85 μl), 2-fluorobenzaldehyde (143 μl) and mercaptosuccinic acid (306 mg) and trimethyl orthoformate (0.5 mL) in THP (3 mL) was heated at 80° C. for 4 hrs. The reaction mixture was cooled, diluted with EtOAc (2 mL) and washed twice with 2 ml of 1N HCl. The organic layer was concentrated to give a residue that was used in the next step without further purification.
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