CN1CCOCC1.[Br:8][C:9]1[S:13][C:12]([C:14]([OH:16])=O)=[CH:11][CH:10]=1.Cl.Cl.[CH3:19][O:20][C:21](=[O:32])[CH:22]([NH:25][C:26]1[N:31]=[CH:30][CH:29]=[CH:28][N:27]=1)[CH2:23][NH2:24].ON1C2C=CC=CC=2N=N1>CN(C=O)C>[CH3:19][O:20][C:21](=[O:32])[CH:22]([NH:25][C:26]1[N:27]=[CH:28][CH:29]=[CH:30][N:31]=1)[CH2:23][NH:24][C:14]([C:12]1[S:13][C:9]([Br:8])=[CH:10][CH:11]=1)=[O:16]4-methylmorpholine (0.23 mL, 2.10 mmol) was added to a mixture of 5-bromothiophene-2-carboxylic acid (124 mg, 0.60 mmol), 3-amino-2-(pyrimidin-2-ylamino)-propionic acid methyl ester bis-hydrochloride salt (161 mg, 0.60 mmol), 1-[3-(dimethylamino)propyl]-3-ethylcarboiimide hydrochloride (115 mg, 0.60 mmol) and 1-hydroxybenzotriazole (81 mg, 0.60 mmol) in dry DMF (2 mL). The mixture was stirred at room temperature overnight. The reaction mixture was concentrated, solvent removed in vacuo and the residue chromatographed. Elution with 5% methanol in dichloromethane gave compound G-2 as a yellow foam (186 mg, 81% yield).
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