YM 273 synthesis

Yield:195883-07-9 96%

Reaction Conditions:

in water; for 1 h;

Steps:

2

Triptolide succinate (20 mg) can be mixed with tris(hydroxymethyl)amino methane (5.3 mg) in 20 ml of water and stirred for one hour. The solution can be filtered and the filtrate lyophilized to yield 24 mg (96%) of white powder. IR(KBr): 3391, 2937.96, 1745.80, 1562.9, 1411.67, 1159, 1066.57, 1024.57 cm^-1. ¹H NMR (D₆-DMSO, ppm): 5.00 (1H, s, 14-CH), 4.85 (2H, d, 19-CH₂), 3.95 (1 H, d, 11-CH), 3.70 (1 H, d, 12-CH), 3.55 (1 H, d, 7-CH), 3.30 (6H, s, 3CH₂O), 2.65 (1 H, m, 5H), 2.45 (2H, m, CH₂), 2.20 (3H, m, CH₂, 15-CH), 1.90 (4H, m, 6-CH₂, 2-CH₂), 1.34 (2H, br, 1-CH₂), 0.95 (3H, s, 20-CH₃), 0.88 (3H, d, 16-CH₃), 0.75 (3H, d, 17-CH₃).

References:

EP1946758,2008,A1 Location in patent:Page/Page column 8