【结 构 式】 |
【分子编号】11886 【品名】1-Methyl-1H-indazole-3-carbonyl chloride 【CA登记号】106649-02-9 |
【 分 子 式 】C9H7ClN2O 【 分 子 量 】194.62016 【元素组成】C 55.54% H 3.63% Cl 18.22% N 14.39% O 8.22% |
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:(II)The synthesis of granisetron has been reported: The reaction of 1-methylindazole-3-carboxylic acid (I) with oxalyl chloride and DMF in dichloromethane gives 1-methylindazole-3-carbonyl chloride (II), which is then condensed with endo-9-methyl-9-azabicyclo[3.3.1]nonan-3-amine (III) by means of triethylamine in dichloromethane.
【1】 GB 2125398 . |
【2】 King, F.D. (SmithKline Beecham plc); Indazolyl carboxylic acid amides useful for treating migraine clusters headache, trigeminal neuralgia or emesis. AU 8656579; EP 0200444; EP 0223385; EP 0498466; ES 8707948; JP 1986275276; JP 1993194508; US 4886808; US 5034398 . |
【3】 King, F.D.; Sanger, G.J.; 5-HT3 RECEPTOR ANTAGONISTS. Drugs Fut 1989, 14, 9, 875. |
【4】 W.D.; Sanger, G.J.; 5-Hydroxytryptamine (5-HT3) receptor antagonists. 1. Indazole and indolizine-3-carboxylic acid derivatives. J Med Chem 1990, 33, 7, 1924-9. |
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) | 11885 | 1-Methyl-1H-indazole-3-carboxylic acid | 50890-83-0 | C9H8N2O2 | 详情 | 详情 |
(II) | 11886 | 1-Methyl-1H-indazole-3-carbonyl chloride | 106649-02-9 | C9H7ClN2O | 详情 | 详情 |
(III) | 11887 | (1R,5S)-1-Amino-9-methyl-9azabicyclo[3.3.1]nonane; (1R,5S)-9-Methyl-9-azabicyclo[3.3.1]non-3-ylamine; (1R,5S)-9-Methyl-9-azabicyclo[3.3.1]nonan-3-amine; 1-Amino-9-methyl-9-azabicyclo[3.3.1]nonane | 76272-56-5 | C9H18N2 | 详情 | 详情 |
Extended Information