反应详情

A solution of 1-(tert-butoxycarbonylamino-methyl)-6,7-dimethoxy-isoquinoline-4-carboxylic acid (100 mg, 0.3 mmol) in 20 mL of THF was treated with 1,2,3,4-tetrahydroisoquinoline (44 mg, 0.33 mmol), TEA (56 mg, 0.552 mmol) and diethyl cyanophosphonate (55 mg, 0.33 mmol) according to the procedure described in example 1E to give [4-(3,4-Dihydro-1H-isoquinoline-2-carbonyl)-6,7-dimethoxy-isoquinolin-1-ylmethyl]-carbamic acid tert-butyl ester (88 mg, 66.9%). H1-NMR (CDCl3): δ, 8.31 (br s, 1H), 7.38 (br s, 1H), 7.15 (m, 5H), 6.82 (m, 1H), 6.18 (br s, 1H), 4.93 (s, 2H), 4.43 (m, 2H), 4.02 (br s, 3H), 3.92 (s, 2H), 3.58 (br s, 3H), 3.10 (br s, 1H), 2.80 (br s, 1H), 1.51 (s, 9H) [Note: broadening of peaks observed due to Boc group, rotamers also observed.]; MS: APCI (M+H) calc'd for C27H31N3O5+H 478.6; found 478.0.