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【结 构 式】 
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【药物名称】YM-274, PG-490-88 【化学名称】4-[(3bS,4aS,5aR,6R,6aS,7aS,7bS,8aS,8bS)-6a-Isopropyl-8b-methyl-1-oxo-1,3,3b,4,4a,6,6a,7a,7b,8b,9,10-dodecahydrotrisoxireno[6,7:8a,9:4b,5]phenanthro[1,2-c]furan-6-yloxy]-4-oxobutyric acid sodium salt 【CA登记号】195883-09-1, 195883-06-8 (free acid), 195883-07-9 (tromethamine salt) 【 分 子 式 】C24H27NaO9 【 分 子 量 】482.46719 |
【开发单位】Duke University (Originator), Pharmagenesis (Originator), Stanford University (Originator), Pierre Fabre (Licensee) 【药理作用】Cystic Fibrosis, Treatment of , IMMUNOMODULATING AGENTS, Oncolytic Drugs, RESPIRATORY DRUGS, Solid Tumors Therapy, Treatment of Transplant Rejection, Antimitotic Drugs |
合成路线1
The title compound is a semisynthetic derivative of triptolide (I), a substance isolated from the root xylem of the Chinese medicinal plant Tripterygium wilfordii. Condensation of (I) with succinic anhydride (II) in hot pyridine furnished the corresponding hemisuccinate ester. This was converted to the corresponding sodium salt by treatment with aqueous NaHCO3 and then isolated by lyophilization of the filtered solution.
| 【1】 Qi, Y.M.; Musser, J.H.; Fidler, J.M. (Pharmagenesis, Inc.); Immunosuppressive cpds. and methods. EP 0907652; JP 2001504437; US 5663335; US 5962516; WO 9731920; WO 9731921 . |
| 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) | 51397 | (3bS,4aS,5aS,6S,6aR,7aS,7bS,8aS,8bS)-6-hydroxy-6a-isopropyl-8b-methyl-3b,4,4a,6,6a,7a,7b,8b,9,10-decahydrotrioxireno[2',3':6,7:2',3':8a,9:2',3':4b,5]phenanthro[1,2-c]furan-1(3H)-one | C20H24O6 | 详情 | 详情 | |
| (II) | 11291 | Dihydro-2,5-furandione; Succinic anhydride | 108-30-5 | C4H4O3 | 详情 | 详情 |