反应详情

Compound 8a was prepared by the same procedure as reported for 6a using 4c (1.00 g, 3.23 mmol), ethyl N-(4-bromobutoxy)ethanimidate49 (924 mg, 3.87 mmol), and DIEA (209 mg, 0.28 mL, 1.6 mmol): yield 635 mg (42%), MS: m/z 467 (M+H)+; 1HNMR (DMSO-d6) δ 7.89 (s, 1H, H-2), 6.87 (q, 1H, 8CH3—NH), 6.46 (bs, 2H, 6-NH2), 5.69 (d, 1H, H-1′, J1′,2′=4.8 Hz), 5.25 (d, 1H, 2′-OH, J2′-2′OH=5.6 Hz), 5.06 (d, 1H, 3′-OH, J3′-3′OH=5.4 Hz), 4.91 (ddd, 1H, H-2′, J1′,2′=4.8 Hz, J2′,3′=5.4 Hz, J2′-2′OH=5.6 Hz), 4.16 (ddd, 1H, H-3′, J2′,3′=5.4 Hz, J3′,4′=4.9 Hz, J3′-3′OH=5.4 Hz), 3.85-3.94 (m, 1H, H-4′), 3.92 (q, 2H, OCH2CH3), 3.80 (t, 2H, NO—CH2), 2.88 (d, 3H, 8NH—CH3, J=4.6 Hz), 2.65-2.74 (m, 1H, 5′-CH2), 2.46-2.58 (m, 1H, 5′-CH2), 2.34 (t, 2H, N(CH3)—CH2), 2.17 (s, 3H, N—CH3), 1.83 (s, 3H, C—CH3), 1.37-1.61 (bm, 4H, NOCH2—CH2CH2), 1.19 (t, 3H, OCH2CH3).