反应详情

The title compound was prepared according to general method B by reaction of N-[(R)-1-(2-benzothiazolyl)thio-2-propyl]-2-bromoadenosine (Example 7) (0.24 g, 0.35 mmol) with 70% w/w aqueous ethylamine (0.23 g) in dioxan (10ml) in a sealed vessel at 100° C. to provide the desired N-[(R)-1-(2-benzothiazolyl)thio-2-propyl]-2-(ethylamino)adenosine as a foam (following column chromatography), 1H NMR (DMSO-d6) δ 1.04 (3H, br t, --NCH2CH3), 1.42 (3H, d, --CHCH3), 3.20 (3H, br m, --NCH2CH3), 3.55-3.80 (4H, m, H-5'a and H-5'b and --CH2 --), 3.95 (1H, q H-4'), 4.15 (1H, q, H-3'), 5.16, 5.41 (2H, 2d, 2'- and 3'-OH), 5.79 (1H, d, H-1'), 6.22 (1H, t, --NHCH2CH3), 7.43, 7.54 (2H, 2 t, Ar-H), 7.98 (1H, s, H-8). HPLC retention time 17.0 min [gradient elution, 20-80% acetonitrile/water (containing 0.1% TFA)].

1. customThe title compound was prepared