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【结 构 式】 
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【药物名称】 【化学名称】2-Ethoxy-3-[4-[2-(4-methyl-1-oxo-1,2-dihydro-2-phthalazinyl)ethoxy]phenyl]propionamide 【CA登记号】221321-60-4 【 分 子 式 】C22H25N3O4 【 分 子 量 】395.46225 |
【开发单位】SSP (Originator) 【药理作用】Antidiabetic Drugs, ENDOCRINE DRUGS, Type 2 Diabetes Mellitus, Agents for, Insulin Sensitizers |
合成路线1
Debenzylation of propanamide (I) by means of H2 over Pd/C in EtOH/HOAc provides alcohol (II), which is then mesylated with methanesulfonyl chloride (MsCl) and Et3N in CH2Cl2 to yield derivative (III). Finally, coupling of (III) with quinazoline derivative (IV) by means of K2CO3 in DMF affords the desired compound.
| 【1】 Ishii, F.; Koya, H.; Honda, H.; Nagao, Y.; Kotake, J.; Konno, F.; Sato, S.; Koda, T.; Ito, Y.; Preparation of benzazine derivatives with hypoglycemic activity. 19th Symp Med Chem (Nov 17 1999, Tokyo) 1999, Abst 1P-05. |
| 【2】 Kotake, J.; Nagao, Y.; Konno, F.; Sato, S.; Honda, H.; Ishii, F. (SSP Co., Ltd.); alpha-Substd. phenylpropionic acid deriv. and medicine containing the same. CA 2247772; EP 0903343; JP 1999158144 . |
| 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) | 45897 | 3-[4-[2-(benzyloxy)ethoxy]phenyl]-2-ethoxypropanamide | C20H25NO4 | 详情 | 详情 | |
| (II) | 45898 | 2-ethoxy-3-[4-(2-hydroxyethoxy)phenyl]propanamide | C13H19NO4 | 详情 | 详情 | |
| (III) | 45899 | 2-ethoxy-3-[4-(2-[[methyl(dimethylene)-lambda(6)-sulfanyl]oxy]ethoxy)phenyl]propanamide | C16H25NO4S | 详情 | 详情 | |
| (IV) | 45900 | 4-methyl-1(2H)-phthalazinone | C9H8N2O | 详情 | 详情 |
Extended Information