反应详情

2-Dimethylamino-1-[7-(3-piperidin-1-yl-propoxy)-3,4-dihydro-1H-isoquinolin-2-yl]-ethanone is prepared from 7-(3-piperidin-1-yl-propoxy)-1,2,3,4-tetrahydro-isoquinoline dihydrochloride (175 mg, 0.5 mmol), PS-DCC (800 mg, 1.1 mmol), HOBt (80 mg, 0.77 mmol), NEt3 (0.21 mL, 1.5 mmol) and N,N-dimethylglycine (1.1 mL, 15 mmol) via a procedure substantially analogous to Procedure E except that PS-trisamine resin beads (700 mg, 2.6 mmol) is used in the work up to scavenge the excess HOBt and N,N-dimethylglycine. The free base product (35 mg, 19% yld) is isolated as an oil. MS(ES+)360.5(M+H)+.

1. customThe free base product (35 mg, 19% yld) is isolated as an oil