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【结 构 式】 
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【分子编号】27636 【品名】4-amino-5-chloro-2-methyl-2,3-dihydro-1-benzofuran-7-carboxylic acid 【CA登记号】 |
【 分 子 式 】C10H10ClNO3 【 分 子 量 】227.64704 【元素组成】C 52.76% H 4.43% Cl 15.57% N 6.15% O 21.08% |
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：(I)The optical resolution of 4-amino-5-chloro-2-methyl-2,3-dihydrobenzofuran-7-carboxylic acid (I) by means of brucine in methanol gives the (+)-isomer (II), which is then condensed with the ethylamino derivative (III) by means of carbonyldiimidazole in THF to afford the amide (IV). Finally, this compound is salified with fumaric acid (V) in ethanol.
| 【1】 Baba, Y.; Usui, T.; Iwata, N. (Sanwa Kagaku Kenkyusho Co., Ltd.); Benzo[b]furancarboxamide derivs., process for their preparation and their use as gastrointestinal mobility-enhancing agents. EP 0640602; JP 1995112985; US 5442077 . |
| 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) | 27636 | 4-amino-5-chloro-2-methyl-2,3-dihydro-1-benzofuran-7-carboxylic acid | C10H10ClNO3 | 详情 | 详情 | |
| (II) | 27634 | (2S)-4-amino-5-chloro-2-methyl-2,3-dihydro-1-benzofuran-7-carboxylic acid | C10H10ClNO3 | 详情 | 详情 | |
| (III) | 19916 | 2-tetrahydro-1H-pyrrolizin-7(5H)-ylethylamine; 2-tetrahydro-1H-pyrrolizin-7(5H)-yl-1-ethanamine | C9H18N2 | 详情 | 详情 | |
| (IV) | 27635 | (2S)-4-amino-5-chloro-2-methyl-N-[2-tetrahydro-1H-pyrrolizin-7(5H)-ylethyl]-2,3-dihydro-1-benzofuran-7-carboxamide | C19H26ClN3O2 | 详情 | 详情 | |
| (V) | 23808 | Fumaric acid; (E)-2-butenedioic acid | 110-17-8 | C4H4O4 | 详情 | 详情 |
Extended Information