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【结 构 式】 
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【药物名称】KUL-7211 【化学名称】(-)-2-[4-[2-[2(R)-Hydroxy-2-(4-hydroxyphenyl)-1(S)-methylethylamino]ethyl]phenoxy]acetic acid 【CA登记号】220129-58-8 【 分 子 式 】C19H23NO5 【 分 子 量 】345.39886 |
【开发单位】Kissei (Originator) 【药理作用】RENAL-UROLOGIC DRUGS, Treatment of Renal Diseases, Urethral Colic, Agents for, Urolithiasis, Agents for, beta2-Adrenoceptor Agonists, beta3-Adrenoceptor Agonists |
合成路线1
The condensation of 4-(2-bromoethyl)phenol (I) with ethyl bromoacetate (II) in the presence of K2CO3 produced the phenoxyacetate (III). This was then condensed with (1R,2S)-2-amino-1-(4-hydroxyphenyl)-propan-1-ol (IV) to give adduct (V). the ethyl ester group of (V) was finally hydrolyzed with NaOH to yield the title carboxylic acid.
| 【1】 Tamai, T.; Akahane, M.; Mukaiyama, H.; Muranaka, H.; Tanaka, N.; Sato, M.; Hirabayashi, A. (Kissei Pharmaceutical Co., Ltd.); Aminoethylphenoxyacetic acid derivs. and drugs for pain remission and calculi removal promotion in urinary lithiasis. EP 1002791; WO 9905090 . |
| 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) | 46834 | 4-(2-bromoethyl)phenol | C8H9BrO | 详情 | 详情 | |
| (II) | 16640 | Ethyl 2-bromoacetate; Ethyl bromoacetate | 105-36-2 | C4H7BrO2 | 详情 | 详情 |
| (III) | 46835 | ethyl 2-[4-(2-bromoethyl)phenoxy]acetate | C12H15BrO3 | 详情 | 详情 | |
| (IV) | 46836 | 4-[(1R,2S)-2-amino-1-hydroxypropyl]phenol | C9H13NO2 | 详情 | 详情 | |
| (V) | 46837 | ethyl 2-[4-(2-[[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl)phenoxy]acetate | C21H27NO5 | 详情 | 详情 |
Extended Information