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【结 构 式】

【分子编号】35067

【品名】(2S)-3-azido-2-hydroxypropyl 4-methylbenzenesulfonate

【CA登记号】

【 分 子 式 】C10H13N3O4S

【 分 子 量 】271.29704

【元素组成】C 44.27% H 4.83% N 15.49% O 23.59% S 11.82%

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)

Alkylation of 1-(2-isopropoxyphenyl)piperazine (I) with 1-azido-3-(p-toluenesulfonyloxy)-2-propanol (II) in hot NMP gave (III). Subsequent hydrogenation of the azido group of (III) over Pd/C provided the intermediate amine (IV).

1 Prouty, C.; Wang, J.; Kuo, G.-H.; Pulito, V.; Murray, W.V.; Cheung, P.; Jolliffe, L.; Varga, S.; Evangelisto, M.; Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: A novel series of potent and selective alpha1a-adrenergic receptor antagonists. J Med Chem 2000, 43, 11, 2183.
2 Murray, W.V.; Kuo, G.-H.; Prouty, C.P. (Ortho-McNeil Pharmaceutical, Inc.); Phthalimido arylpiperazines as alpha 1a receptor antagonists useful in the treatment of benign prostatic hyperplasia. US 6063785; WO 9942445 .
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) 35066 isopropyl 2-(1-piperazinyl)phenyl ether; 1-(2-isopropoxyphenyl)piperazine C13H20N2O 详情 详情
(II) 35067 (2S)-3-azido-2-hydroxypropyl 4-methylbenzenesulfonate C10H13N3O4S 详情 详情
(III) 35068 (2R)-1-azido-3-[4-(2-isopropoxyphenyl)-1-piperazinyl]-2-propanol C16H25N5O2 详情 详情
(IV) 35069 (2S)-1-amino-3-[4-(2-isopropoxyphenyl)-1-piperazinyl]-2-propanol C16H27N3O2 详情 详情
Extended Information