反应详情

A solid mixture of N-(4-amino-5-benzothiazol-2-yl-5-oxo-pentyl)-guanidine (0.24 g, 0.83 mmol) and 1-acetyl-4-hydroxy-pyrrolidine-2-carboxylic acid (0.14 g, 0.83 mmol) was dissolved in THF (10 mL) and water (2 mL). To the reaction mixture was then added N,N′-diisopropyl carbodiimide to yield a reaction mixture of pH 1.8 at 0° C. The pH of the reaction mixture was adjusted to about 5.5 with 8% NaHCO3. The reaction mixture was stirred at ambient temperature for 4 hours. The title compound was detected by HPLC (180 mg) and assayed by weight analysis.