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【结 构 式】 
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【药物名称】Vadocaine hydrochloride, K-242-HCl, ORK-242-HCl 【化学名称】2',4'-Dimethyl-6'-methoxy-3-(2-methylpiperidino)propionanilide hydrochloride 【CA登记号】72005-58-4 (free base) 【 分 子 式 】C18H29ClN2O2 【 分 子 量 】340.89703 |
【开发单位】Orion Corp. (Originator) 【药理作用】Antitussives, RESPIRATORY DRUGS, Treatment of Upper Respiratory Tract Disorders |
合成路线1
The condensation of 3-chloropropionyl chloride (I) with 2,4 dimethyl-6 methoxyaniline (II) by means of sodium acetate in glacial acetic acid gives 3-chloro-N-(2,4-dimethyl-6-methoxyphenyl)propionamide (III), which is condensed with 2-methylpiperidine (IV) in refluxing anhydrous benzene.
| 【1】 Kaila, J.O.W.; Honkanen, E.J.; Alberty, J.E.; Hukki, J.J. (Orion Corporation); Novel anilides, their process of preparation and t. BE 0873957; US 4353914 . |
| 【2】 Prous, J.; Castaner, J.; Vadocaine hydrochloride. Drugs Fut 1988, 13, 10, 936. |
| 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) | 18936 | 3-chloropropanoyl chloride | 625-36-5 | C3H4Cl2O | 详情 | 详情 |
| (II) | 23099 | 2-methoxy-4,6-dimethylphenylamine; 2-methoxy-4,6-dimethylaniline | C9H13NO | 详情 | 详情 | |
| (III) | 23100 | 3-chloro-N-(2-methoxy-4,6-dimethylphenyl)propanamide | C12H16ClNO2 | 详情 | 详情 | |
| (IV) | 23101 | 2-methylpiperidine | 3197-42-0 | C6H13N | 详情 | 详情 |
Extended Information