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【结 构 式】

【分子编号】38677

【品名】(2R)-2-(1H-imidazol-1-yl)-2-phenyl-1-ethanamine; (2R)-2-(1H-imidazol-1-yl)-2-phenylethylamine

【CA登记号】

【 分 子 式 】C11H13N3

【 分 子 量 】187.24444

【元素组成】C 70.56% H 7% N 22.44%

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:(X)

The esterification of 2(S)-amino-2-phenylethanol (VII) with hot sulfuric acid gives the expected O-sulfate (VIII), which by treatment with hot aqueous NaOH yields the aziridine (IX). The condensation of (IX) with imidazole (VI) by heating at 120 C affords 2(R)-(1-imidazolyl)-2-phenylethan-1-amine (X). Finally, this compound is condensed with 4'-chlorobiphenyl-4-thiocarboxylic acid 2-pyridylthioester in DMF.

1 Schuster, I.; Egger, H. (Novartis AG; Novartis Deutschland GmbH); Acylated aminoalkanimidazoles and -triazoles. CA 2149459; EP 0683156; JP 1996053422; US 5622982 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(VI) 10255 Imidazole; 1H-Imidazole 288-32-4 C3H4N2 详情 详情
(VII) 10973 (2S)-2-Amino-2-phenyl-1-ethanol; (S)-2-Hydroxy-1-phenylethylamine; (S)-(+)-2-Phenylglycinol; (S)-2-Amino-2-phenyl-1-ethanol 20989-17-7 C8H11NO 详情 详情
(VIII) 38675 (2S)-2-amino-2-phenylethyl hydrogen sulfate C8H11NO4S 详情 详情
(IX) 38676 (2S)-2-phenylaziridine C8H9N 详情 详情
(X) 38677 (2R)-2-(1H-imidazol-1-yl)-2-phenyl-1-ethanamine; (2R)-2-(1H-imidazol-1-yl)-2-phenylethylamine C11H13N3 详情 详情
(XI) 38678 S-(2-pyridinyl) 4'-chloro[1,1'-biphenyl]-4-carbothioate C18H12ClNOS 详情 详情
Extended Information