【结 构 式】 |
【分子编号】52997 【品名】2-fluoro-5-nitrobenzoyl chloride 【CA登记号】n/a |
【 分 子 式 】C7H3ClFNO3 【 分 子 量 】203.5568632 【元素组成】C 41.3% H 1.49% Cl 17.42% F 9.33% N 6.88% O 23.58% |
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)2-Fluoro-5-nitrobenzoic acid (I) was converted to the corresponding acid chloride (II) by chlorination of with SOCl2. Condensation of acid chloride (II) with 3,4-dimethoxybenzylamine (III) provided amide (IV). The aromatic fluorine atom of (IV) was then displaced with (R)-2-amino-1-propanol (V) in hot pyridine to furnish the title anthranilic acid derivative.
【1】 Oku, T.; Sawada, K.; Kuroda, A.; Kayakiri, N.; Sawada, Y.; Inoue, T.; Mizutani, T. (Fujisawa Pharmaceutical Co., Ltd.); Anthranilic acid derivs. as inhibitors of the cGMP-phosphodiesterase. EP 1080069; JP 2001508811; US 6384080; WO 9954284 . |
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) | 52996 | 2-Fluoro-5-nitrobenzoic acid | 320-98-9 | C7H4FNO4 | 详情 | 详情 |
(II) | 52997 | 2-fluoro-5-nitrobenzoyl chloride | n/a | C7H3ClFNO3 | 详情 | 详情 |
(III) | 13920 | (3,4-Dimethoxyphenyl)methanamine; 3,4-Dimethoxybenzylamine; Veratrylamine | 5763-61-1 | C9H13NO2 | 详情 | 详情 |
(IV) | 52998 | N-(3,4-dimethoxybenzyl)-2-fluoro-5-nitrobenzamide | n/a | C16H15FN2O5 | 详情 | 详情 |
(V) | 21414 | (2R)-2-Amino-1-propanol; D-Alaninol; D-(-)-Alaninol | 35320-23-1 | C3H9NO | 详情 | 详情 |
Extended Information