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【结 构 式】

【分子编号】28022

【品名】(2S)-1-acetyl-2-pyrrolidinecarboxylic acid

【CA登记号】68-95-1

【 分 子 式 】C7H11NO3

【 分 子 量 】157.16928

【元素组成】C 53.49% H 7.05% N 8.91% O 30.54%

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)

Optically active sulpiride is prepared by converting levo-proline (I) to the correspondig levorotatory acetylproline (II), followed by reduction, chlorination and amination to afford levorotatory N-ethyl-2-aminomethylpyrrolidine (V), which, upon treatment with an ester of 2-methoxy-5-sulfamoylbenzoic acid (VI), yields N-(1-ethyl-2-pyrrolidinomethyl)-2-methoxy-5-sulfamoylbenzamide, that is, the levorotatory enantiomer of sulpiride.

1 Forgione, A.; Levosulpiride. Drugs Fut 1987, 12, 10, 944.
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) 16731 L-proline 147-85-3 C5H9NO2 详情 详情
(II) 28022 (2S)-1-acetyl-2-pyrrolidinecarboxylic acid 68-95-1 C7H11NO3 详情 详情
(III) 28023 [(2S)-1-ethylpyrrolidinyl]methanol C7H15NO 详情 详情
(IV) 28024 (2S)-2-(chloromethyl)-1-ethylpyrrolidine C7H14ClN 详情 详情
(V) 21345 (2S)-1-Ethyl-2-(aminomethyl)pyrrolidine; [(2S)-1-Ethylpyrrolidinyl]methanamine C7H16N2 详情 详情
(VI) 28025 methyl 5-(aminosulfonyl)-2-methoxybenzoate 33045-52-2 C9H11NO5S 详情 详情
Extended Information