反应详情

The title compound was prepared following the method described above for the synthesis of 4-((1R,3aS,5aR,5bR,7aR,11aS,11bR,13aR,13bR)-3a-(2-(dimethylamino)-2-oxoethylamino)-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)benzoic acid using 4-(2-chloroethyl)thiomorpholine hydrochloride (prepared as describe in WO 2009058859) as the alkylating reagent in Step 1. The product was isolated as a white solid (3 mg, 0.85%). LCMS: m/e 659.37 (M+H)+, 2.38 min (method 13). 1H NMR (400 MHz, CHLOROFORM-d) δ 8.00 (d, J=8.3 Hz, 2H), 7.21 (d, J=8.5 Hz, 2H), 5.32-5.19 (m, 1H), 4.77 (s, 1H), 4.65 (s, 1H), 3.11-2.98 (m, 1H), 2.89 (m, 5H), 2.75 (m, 5H), 2.67-2.57 (m, 1H), 2.31-2.16 (m, 1H), 2.14-1.85 (m, 6H), 1.71 (s, 7H), 1.59-1.40 (m, 6H), 1.38-1.15 (m, 8H), 1.08-0.96 (m, 10H), 0.94 (s, 3H)