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【结 构 式】 
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【分子编号】34333 【品名】2-[4-(2-aminoethyl)phenoxy]acetic acid 【CA登记号】 |
【 分 子 式 】C10H13NO3 【 分 子 量 】195.21816 【元素组成】C 61.53% H 6.71% N 7.17% O 24.59% |
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：(IV)The reaction of 4-[2-(acetylamino)ethyl]phenol (I) with ethyl bromoacetate (II) by means of K2CO3 in refluxing butanone gives 4-[2-(acetylamino)ethyl]phenoxyacetic acid ethyl ester (III), which is hydrolyzed with refluxing aqueous HCl to 4-(2-aminoethyl)phenoxyacetic acid (IV). Finally, this compound is acylated with benzenesulfonyl chloride (V) by means of K2CO3 in hot water.
| 【1】 Witte, E.C.; Wolff, H.P.; Thiel, M.; Stegmeier, K.; Roesch, E.; Phenoxyalkylcarboxylic acid compounds and thrombocyte-aggregation inhibition. DE 2809377; EP 0004011; ES 478228; JP 54122250; US 4258058 . |
| 【2】 Karup, G.L.; Preikschat, H.F. (GEA A/S Farmaceutisk Fabrik); Process for the preparation of 1,4-dihydropyridines and cpds. used in this process. WO 9925688 . |
| 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) | 19989 | N-(4-hydroxyphenethyl)acetamide | C10H13NO2 | 详情 | 详情 | |
| (II) | 16640 | Ethyl 2-bromoacetate; Ethyl bromoacetate | 105-36-2 | C4H7BrO2 | 详情 | 详情 |
| (III) | 34332 | ethyl 2-[4-[2-(acetamido)ethyl]phenoxy]acetate | C14H19NO4 | 详情 | 详情 | |
| (IV) | 34333 | 2-[4-(2-aminoethyl)phenoxy]acetic acid | C10H13NO3 | 详情 | 详情 | |
| (V) | 14713 | benzenesulfonyl chloride | 98-09-9 | C6H5ClO2S | 详情 | 详情 |
Extended Information