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【结 构 式】 
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【药物名称】 【化学名称】N-(6-Amino-3-methyl-2,4-dioxo-1-phenyl-1,2,3,4-tetrahydropyrimidin-5-yl)-3-(3,5-di-tert-butyl-4-hydroxyphenyl)-2-propenamide 【CA登记号】 【 分 子 式 】C28H34N4O4 【 分 子 量 】490.60758 |
【开发单位】Japan Energy (Originator) 【药理作用】Allergic Skin Disorders, Treatment for, DERMATOLOGIC DRUGS, Non-Steroidal Antiinflammatory Drugs |
合成路线1
Nitrosation of pyrimidinedione (I) with NaNO2/HCl affords (II), which is further reduced to the diaminopyrimidine (III) by catalytic hydrogenation over Pd/C. Subsequent coupling of (III) with 2,6-di-tert-butyl-4-hydroxycinnamic acid (IV) employing DPP-Cl furnishes the title amide
| 【1】 Isobe, Y.; Tobe, M.; Inoue, Y.; Goto, Y.; Obara, F.; Isobe, M.; Hayashi, H.; Inhibitory activities of novel pyrimidine derivatives on the contact hypersensitivity reaction. Chem Pharm Bull 2003, 51, 3, 309. |
| 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) | 44183 | 6-amino-3-methyl-1-phenyl-2,4(1H,3H)-pyrimidinedione | C11H11N3O2 | 详情 | 详情 | |
| (II) | 63475 | 6-amino-3-methyl-5-nitroso-1-phenyl-2,4(1H,3H)-pyrimidinedione | C11H10N4O3 | 详情 | 详情 | |
| (III) | 44185 | 5,6-diamino-3-methyl-1-phenyl-2,4(1H,3H)-pyrimidinedione | C11H12N4O2 | 详情 | 详情 | |
| (IV) | 43375 | (E)-3-[3,5-di(tert-butyl)-4-hydroxyphenyl]-2-propenoic acid | 22014-01-3 | C17H24O3 | 详情 | 详情 |
Extended Information