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【结 构 式】 
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【药物名称】 【化学名称】4-(2,2-Dimethyl-1-oxopropyl)benzoic acid 2-[4-(2,2-dimethyl-1-oxopropyl)benzoyloxymethyl]-1,4-butanediyl diester 【CA登记号】328397-37-1 【 分 子 式 】C41H48O9 【 分 子 量 】684.83431 |
【开发单位】Novartis (Originator) 【药理作用】Antidiabetic Drugs, Chemical Delivery Systems, DRUG DELIVERY, Drug Delivery Systems, ENDOCRINE DRUGS, Type 2 Diabetes Mellitus, Agents for, Glucose Lowering Agents |
合成路线1
Treatment of 4-(2,2-dimethyl-1-oxopropyl)benzoic acid (I) with thionyl chloride afforded the corresponding acid chloride (II). The title triester was then obtained by acylation of 2-(hydroxymethyl)-1,4-butanediol (IV) with acid chloride (II) in the presence of DMAP or Et3N. The triol (IV) has been obtained by reduction of ethane-1,1,2-tricarboxylic acid triethyl ester (III) with LiAlH4 under standard conditions.
| 【1】 Otero, D.A.; Bebernitz, G.R.; Dain, J.G.; Strohschein, R.J.; Deems, R.O.; Simpson, W.R.; Reduction in glucose levels in STZ diabetic rats by 4-(2,2-dimethyl-1-oxopropyl)benzoic acid: A prodrug approach for targeting the liver. J Med Chem 2001, 44, 4, 512. |