【结 构 式】 |
【分子编号】12855 【品名】(E)-6-(4-Hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-4-hexenoyl chloride 【CA登记号】 |
【 分 子 式 】C17H19ClO5 【 分 子 量 】338.78756 【元素组成】C 60.27% H 5.65% Cl 10.46% O 23.61% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号:(II)Commercially available mycophelonic acid (I) is converted to its chloride (II) by means of thionyl chloride in dichloromethane/DMF and then esterified with 2-(4-morpholinyl)ethanol (III) in dichloromethane.
【1】 Robinson, C.; Castaner, J.; Mycophenolate Mofetil. Drugs Fut 1995, 20, 4, 356. |
【2】 Allison, A.C.; Eugui, E.M.; Nelson, P.H.; Gu, C.-L.L.; Lee, W.A. (Syntex (USA), Inc.); Treatment of allograft rejection with mycophenolic acid morpholinoethyl ester and derivs. Thereof. US 4786637 . |
【3】 Nelson, P.H.; Gu, C.-L.L.; Allison, A.C.; Eugui, E.M.; Lee, W.A. (Syntex (USA), Inc.); Morpholinoethylesters of mycophenolic acid and pharmaceutical compsns. AU 8782540; EP 0281713; JP 1988188672; US 4753935 . |
【4】 Leung, K.; Nelson, P.H.; Miksztal, A.R.; Lee, W.A.; Gu, L.; Chu, N.; Bioavailability improvement of mycophenolic acid through amino ester derivatization. Pharm Res 1990, 7, 2, 161-6. |
中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
---|---|---|---|---|---|---|
(I) | 12854 | Mycophenolic acid; (E)-6-(4-Hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-4-hexenoic acid | 483-60-3 | C17H20O6 | 详情 | 详情 |
(II) | 12855 | (E)-6-(4-Hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-4-hexenoyl chloride | C17H19ClO5 | 详情 | 详情 | |
(III) | 12856 | 4-(2-Hydroxyethyl)morpholine; 2-(4-Morpholinyl)-1-ethanol; N-(2-Hydroxyethyl)morpholine | 622-40-2 | C6H13NO2 | 详情 | 详情 |
Extended Information