【结 构 式】 |
【分子编号】49555 【品名】1-[3-(4-fluorophenoxy)propyl]-3-methoxy-4-piperidinone 【CA登记号】 |
【 分 子 式 】C15H20FNO3 【 分 子 量 】281.3271432 【元素组成】C 64.04% H 7.17% F 6.75% N 4.98% O 17.06% |
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 reductive amination of 1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-one (I) with benzylamine by hydrogenation with H2 over Pd/C, followed by crystallization of the HCl or HNO3 salts, gives cis-1-[3-(4-fluorophenyl)propyl]-3-methoxypiperidine-4-amine (II). This compound is condensed with 4-amino-5-chloro-2-methoxybenzoic acid (III) by means of ethyl chloroformate, TEA and HOBt to afford the target amide.
【1】 Moens, L.J.R.; Rey, M.; De Knaep, A.G.M. (Janssen Pharmaceutica NV); Synthesis of cisapride. WO 9816511 . |
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) | 49555 | 1-[3-(4-fluorophenoxy)propyl]-3-methoxy-4-piperidinone | C15H20FNO3 | 详情 | 详情 | |
(II) | 49554 | (3S,4R)-1-[3-(4-fluorophenoxy)propyl]-3-methoxy-4-piperidinamine; (3S,4R)-1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidinylamine | C15H23FN2O2 | 详情 | 详情 | |
(III) | 12419 | 4-Amino-5-chloro-2-methoxybenzoic acid | 7206-70-4 | C8H8ClNO3 | 详情 | 详情 |
Extended Information