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General procedure: To a solution of 7a (450 mg, 1.50 mmol), 1-(4-chloroisoquinolin-1-yl)piperazine (446 mg, 1.80 mmol) and acetic acid (0.090 mL, 1.6 mmol) in 1,2-dichloroethane (8 mL) was added sodium triacetoxyborohydride (636 mg, 3.00 mmol) and the mixture was stirred at room temperature for 3 h. The reaction mixture was poured into a saturated aqueous sodium hydrogen carbonate solution and extracted with chloroform. The extract was washed with brine, dried and concentrated under reduced pressure. The residue purified by silica gel chromatography with chloroform/methanol (50:1, v/v) to give 3-{(2S,4S)-1-tert-butoxycarbonyl-4-[4-(4-chloroisoquinolin-1-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl}thiazolidine (596 mg, 75%) as a white powder.The above compound (592 mg, 1.11 mmol) was dissolved in 1.1 mol/L hydrogen chloride in methanol (10 mL), and the mixture was stirred at room temperature for 5 days. The reaction mixture was concentrated under reduced pressure, and the residue was crystallized with ethanol to give the title compound (318 mg, 52%) as a pale-yellow powder.
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