【结 构 式】 |
【分子编号】28152 【品名】4-amino-5-chloro-2-methoxybenzoyl chloride 【CA登记号】 |
【 分 子 式 】C8H7Cl2NO2 【 分 子 量 】220.05452 【元素组成】C 43.67% H 3.21% Cl 32.22% N 6.37% O 14.54% |
与该中间体有关的原料药合成路线共 2 条
合成路线1
该中间体在本合成路线中的序号:(III)By condensation of 4-amino-5-chloro-2-methoxybenzoyl chloride (III) with 4-amino-1-[3-(fluorophenoxy)propyl]-3-methoxypiperidine (IV) by means of triethylamine in CHCl3.
【1】 Van Daele, G. (Janssen Pharmaceutica NV); Novel N-(3-hydroxy-4-piperidinyl)benzamide derivs.. US 4962115 . |
【2】 Neuman, M.; Serradell, M.N.; Castaner, J.; Cisapride. Drugs Fut 1984, 9, 7, 497. |
合成路线2
该中间体在本合成路线中的序号:(IV)The reaction of 1-azabicyclo[3.3.1]nonan-4-one (I) with hydroxyamine gives the corresponding oxime (II), which is reduced with LiAlH4 in THF yielding 4-amino-1-azabicyclo [3.3.1]nonane (III). Finally, this compound is condensed with 4-amino-5-chloro-2-methoxybenzoylchloride (IV).
【1】 King, F.D. (SmithKline Beecham plc); Azabicyclo compounds, useful as intermediates. EP 0094742; JP 5194513; JP 58188885; US 4857647 . |
【2】 Serradell, M.N.; Castaner, R.M.; Castaner, J.; BRL-24924. Drugs Fut 1987, 12, 11, 1009. |
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) | 11627 | 1-Azabicyclo[3.3.1]nonan-4-one | C8H13NO | 详情 | 详情 | |
(II) | 11628 | 1-Azabicyclo[3.3.1]nonan-4-one oxime | C8H14N2O | 详情 | 详情 | |
(III) | 11629 | (R)-1-Azabicyclo[3.3.1]non-4-ylamine; (R)-1-Azabicyclo[3.3.1]nonan-4-amine | C8H16N2 | 详情 | 详情 | |
(IV) | 28152 | 4-amino-5-chloro-2-methoxybenzoyl chloride | C8H7Cl2NO2 | 详情 | 详情 |
Extended Information