Tryptophan hydroxylase-1 inhibitor ursolic acid derivatives as well as preparation method and application thereof
A technology of tryptophan hydroxylase and ursolic acid, which is applied in the direction of steroids, organic chemistry, drug combination, etc., to increase the bone density of the spine and prevent osteoporosis
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Embodiment 1
[0041] The preparation of compound 2, reaction formula is:
[0042]
[0043]Weigh 13.25g (28.8mmol) ursolic acid and dissolve it in 150.0mL N,N-dimethylacetamide or N,N-dimethylformamide at 90°C, slowly add 10.0mL hydrogen peroxide / sodium tungstate / Disodium hydrogen phosphate / sodium dihydrogen phosphate (12.5 / 0.5 / 0.2 / 0.2, molar equivalent) mixed solution, control the dropping time at about 1 hour. After reacting for one hour, it was cooled, poured into cold water, extracted with ethyl acetate, washed, dried over anhydrous sodium sulfate, and evaporated to obtain 3.92 g of 3-carbonyl ursolic acid 2, yield: 86%. Product characterization, the data are: 1 H NMR (300MHz, CDCl 3 )δ: 5.30(s, 1H), 2.76(d, J=15.0Hz, 1H), 2.28–2.14(m, 3H), 2.09–1.97(m, 2H), 1.84–1.69(m, 3H), 1.64 –1.47(m, 6H), 1.33(d, J=2.8Hz, 3H), 1.31(s, 2H), 1.28(d, J=2.1Hz, 3H), 1.23(s, 3H), 1.18(s, 3H), 0.99(s, 3H), 0.97(s, 2H), 0.95(s, 4H), 0.83(s, 3H). 13 CNMR (75MHz, CDCl 3 )δ: 178.1, 142.4, 138.9, 134...
Embodiment 2
[0443] Embodiment 2 ursolic acid derivative concrete experimental example:
[0444] 1) In vitro inhibition of 5-HT synthesis experiment
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