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【结 构 式】 
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【药物名称】Dinazafone, F-1797 【化学名称】N1-(2-Benzoyl-4-chlorophenyl)-N1-methyl-N2-(2-methyl-2-propenyl)glycinamide 【CA登记号】71119-12-5 【 分 子 式 】C20H21ClN2O2 【 分 子 量 】356.85557 |
【开发单位】 【药理作用】 |
合成路线1
The tosylation of 2-amino-5-chlorobenzophenone (I) with tosyl chloride (II) in pyridine gives 2-tosylamido-5-chlorobenzophenone (III), which is methylated with dimethyl sulfate and sodium methoxide in toluene yielding N-methyl-2-tosylamido-5-chlorobenzophenone (IV). Hydrolysis of (IV) with aqueous sulfuric acid affords 2-methylamino-5-chlorobenzophenone (V), which is acylated with bromoacetyl chloride (VI) in benzene to give N-methyl-2-(bromoacetylamido)-5-chlorobenzophenone (VII). Finally this compound is condensed with 2-methylallylamine (VIII) in acetone
| 【1】 Mouzin, G.; Cousse, H.; Stenger, A.; Casadio, S. (Pierre Fabre S.A.); US 4372975 . |
| 【2】 Serradell, M.N.; Castaner, J.; Souto, M.; Dinazafone. Drugs Fut 1984, 9, 7, 501. |
| 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) | 10279 | (2-Amino-5-chlorophenyl)(phenyl)methanone; 2-Amino-5-chlorobenzophenone | 719-59-5 | C13H10ClNO | 详情 | 详情 |
| (II) | 25151 | phenylmethanesulfonyl chloride | 1939-99-7 | C7H7ClO2S | 详情 | 详情 |
| (III) | 61085 | N-(2-benzoyl-4-chlorophenyl)(phenyl)methanesulfonamide | C20H16ClNO3S | 详情 | 详情 | |
| (IV) | 61086 | N-(2-benzoyl-4-chlorophenyl)-N-methylphenylmethanesulfonamide | C21H18ClNO3S | 详情 | 详情 | |
| (V) | 33972 | [5-chloro-2-(methylamino)phenyl](phenyl)methanone | 1022-13-5 | C14H12ClNO | 详情 | 详情 |
| (VI) | 27903 | 2-Bromoacetyl chloride | 22118-09-8 | C2H2BrClO | 详情 | 详情 |
| (VII) | 33973 | N-(2-benzoyl-4-chlorophenyl)-2-bromo-N-methylacetamide | C16H13BrClNO2 | 详情 | 详情 | |
| (VIII) | 61087 | 2-methyl-2-propen-1-amine; 2-methyl-2-propenylamine | C4H9N | 详情 | 详情 |
Extended Information