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【结 构 式】 
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【分子编号】21858 【品名】(7R)-3-[(acetoxy)methyl]-7-[[2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(methoxyimino)acetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid 【CA登记号】 |
【 分 子 式 】C15H16N6O7S2 【 分 子 量 】456.46028 【元素组成】C 39.47% H 3.53% N 18.41% O 24.54% S 14.05% |
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 reaction of 7beta-[2-(5-amino-1,2,4-thiadiazol-3-yl)-2(Z)-(methoxyimino)acetamido]-3-acetoxymethyl-3-cephem-4-carboxylic acid (I) with N-methyl-N-(trimethylsilyl)trifluoroacetamide and then with iodotrimethylsilane in dichloromethane gives the corresponding silylated 3-iodomethyl derivative (II), which is then treated with 4-carbamoylquinuclidine (III) in acetonitrile.
| 【1】 Kamiya, T.; Machida, Y.; Negi, S.; Nomoto, S.; Saito, I.; Sugiyama, I.; Yamauchi, H. (Eisai Co., Ltd.); Cephem cpds. having at the 3-position a (1,4-methylene-1-piperidinio)methyl group or a (1-quinuclidinio)methyl group. AU 8652240; EP 0188255; ES 8703885; JP 1987030786; JP 1987123189; US 4748171; US 5010188 . |
| 【2】 Prous, J.; Castaner, J.; E-1040. Drugs Fut 1988, 13, 2, 117. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| 21859 | 2,2,2-trifluoro-N-methyl-N-(trimethylsilyl)acetamide | C6H12F3NOSi | 详情 | 详情 | ||
| (I) | 21858 | (7R)-3-[(acetoxy)methyl]-7-[[2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(methoxyimino)acetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid | C15H16N6O7S2 | 详情 | 详情 | |
| (II) | 21860 | trimethylsilyl (7R)-3-(iodomethyl)-7-[(2-(methoxyimino)-2-[5-[(trimethylsilyl)amino]-1,2,4-thiadiazol-3-yl]acetyl)amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate | C19H29IN6O5S2Si2 | 详情 | 详情 | |
| (III) | 11766 | 4-Quinuclidinecarboxamide | C8H14N2O | 详情 | 详情 |
Extended Information