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【结 构 式】 
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【药物名称】Thionisoxetine-(R), (R)-Thionisoxetine, LY-368975 【化学名称】(R)-N-Methyl-3-[2-(methylsulfanyl)phenoxy]-3-phenylpropylamine hydrochloride 【CA登记号】 【 分 子 式 】C17H22ClNOS 【 分 子 量 】323.88799 |
【开发单位】Lilly (Originator) 【药理作用】Antiobesity Drugs, METABOLIC DRUGS, Treatment of Eating Disorders, Treatment of Nutritional Disorders, Norepinephrine Reuptake Inhibitors |
合成路线1
Reduction of 3-chloropropiophenone (I) with NaBH4 produced 3-chloro-1-phenyl-1-propanol (II). Subsequent Mitsunobu coupling of (II) with 2-(methylthio)phenol (III) in the presence of DEAD and PPh3 afforded ether (IV). Finally, substitution of the halogen of (IV) for methylamine provided the corresponding secondary amine.
| 【1】 Gehlert, D.R.; Robertson, D.W.; Wong, D.T. (Eli Lilly and Company); N-Alkyl-3-phenyl-3-(2-alkylthiophenoxy)propylamines. EP 0591581 . |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| 11021 | Methanamine; Methylamine | 74-89-5 | CH5N | 详情 | 详情 | |
| (I) | 28073 | 3-chloro-1-phenyl-1-propanone | 936-59-4 | C9H9ClO | 详情 | 详情 |
| (II) | 28074 | 3-chloro-1-phenyl-1-propanol | C9H11ClO | 详情 | 详情 | |
| (III) | 28075 | 2-(methylsulfanyl)phenol | 1073-29-6 | C7H8OS | 详情 | 详情 |
| (IV) | 28076 | 1-(3-chloro-1-phenylpropoxy)-2-(methylsulfanyl)benzene | C16H17ClOS | 详情 | 详情 |
Extended Information