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【结 构 式】

【分子编号】26533

【品名】2-bromoethyl 4-amino-5-chloro-2-methoxybenzoate

【CA登记号】

【 分 子 式 】C10H11BrClNO3

【 分 子 量 】308.55898

【元素组成】C 38.93% H 3.59% Br 25.9% Cl 11.49% N 4.54% O 15.56%

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)

Reaction of 4-amino-5-chloro-2-methoxybenzoic acid (I) with 1,2-dibromoethane in the presence of 1,8-diazabicyclo[5.4.0]undec-7-ene afforded bromoethyl ester (II). This was then condensed with a mixture of cis and trans 3,5-dimethylpiperidines (III), and the resulting mixture of amines was finally separated by column chromatogaphy to provide the target cis compound.

1 Sicsic, S.; Soulier, J.-L.; Yang, D.; et al.; New esters of 4-amino-5-chloro-2-methoxybenzoic acid as potent agonists and antagonists for 5-HT4 receptors. J Med Chem 1997, 40, 4, 608.
2 Langlois, M.; Guzzi, U.; Cecchi, R.; Croci, T. (Midy SpA); Esters of 4-amino-5-chloro-2-methoxybenzoic acid, process for their preparation and pharmaceutical compsns. containing them. EP 0683161 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
10252 1,2-Dibromoethane; Ethylene dibromide 106-93-4 C2H4Br2 详情 详情
(I) 12419 4-Amino-5-chloro-2-methoxybenzoic acid 7206-70-4 C8H8ClNO3 详情 详情
(II) 26533 2-bromoethyl 4-amino-5-chloro-2-methoxybenzoate C10H11BrClNO3 详情 详情
(III) 26534 3,5-dimethylpiperidine 35794-11-7 C7H15N 详情 详情
Extended Information