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【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