反应详情

The title compound was prepared following the method described in step 1 for the preparation of Example 1, using (1R,3aS,5aR,5bR,7aR,11aR,11bR,13aR,13bR)-3a-((2-(1,1-dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1H-cyclopenta[a]chrysen-9-yl trifluoromethanesulfonate and ethyl 2-methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-4H-1,3-dioxine-2-carboxylate as the reactants. The product was isolated as a mixture of diasteromers in 13.3% yield. MS: m/e 741.55 (M+H)+, 2.72 min (method 8). 1H NMR (400 MHz, CHLOROFORM-d) δ 6.35-6.30 (m, 1H), 5.36 (d, J=5.5 Hz, 1H), 4.73 (s, 1H), 4.60 (s, 1H), 4.42 (ddd, J=15.4, 7.6, 1.4 Hz, 1H), 4.33-4.21 (m, 2H), 4.20-4.12 (m, 1H), 3.14-3.00 (m, 11H), 2.80-2.47 (m, 2H), 2.12-1.73 (m, 2H), 1.69 (s, 3H), 1.62 (s, 3H), 1.55-1.19 (m, 11H), 1.10-1.02 (m, 12H), 1.00-0.94 (m, 6H), 0.92-0.87 (m, 3H), 0.86-0.78 (m, 6H).

1. customdescribed in step 1 for the preparation of Example 1
2. customThe product was isolated as a mixture of diasteromers in 13.3% yield
3. customm/e 741.55 (M+H)+, 2.72 min (method 8)