Cl.[Cl:2][C:3]1[CH:8]=[C:7]([Cl:9])[CH:6]=[CH:5][C:4]=1[C:10]1[NH:15][C:14](=[O:16])[N:13]2[N:17]=[C:18]([CH:20]3[CH2:25][CH2:24][NH:23][CH2:22][CH2:21]3)[N:19]=[C:12]2[CH:11]=1.[CH2:26]=O.[Na]>CO>[Cl:2][C:3]1[CH:8]=[C:7]([Cl:9])[CH:6]=[CH:5][C:4]=1[C:10]1[NH:15][C:14](=[O:16])[N:13]2[N:17]=[C:18]([CH:20]3[CH2:25][CH2:24][N:23]([CH3:26])[CH2:22][CH2:21]3)[N:19]=[C:12]2[CH:11]=1At 0° C., 500 mg (1.25 mmol) of 7-(2,4-dichlorophenyl)-2-(piperidin-4-yl)[1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-one hydrochloride were initially charged in methanol (4 ml), and 3 Å molecular sieve (50 mg), formalin (210 μl, 7.50 mmol) and sodium cyanoborhydride (470 mg, 7.50 mmol) were added. The mixture was stirred at 0° C. for 1 h and then stirred at RT for another 12 h. The reaction mixture was filtered, and dichloromethane (100 ml) and water (75 ml) were added to the filtrate. The mixture was extracted and the organic phase was dried (magnesium sulfate) and concentrated. This gave 274 mg (58% of theory) of the crude product.
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