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【结 构 式】 
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【药物名称】KC-764 【化学名称】2-Methyl-3-(1,4,5,6-tetrahydronicotinoyl)pyrazolo[1,5-a]pyridine 【CA登记号】94457-09-7 【 分 子 式 】C14H15N3O 【 分 子 量 】241.29515 |
【开发单位】Kyorin (Originator) 【药理作用】Antiplatelet Therapy, Coagulation Disorders Therapy, HEMATOLOGIC DRUGS, Cyclooxygenase Inhibitors |
合成路线1
The reaction of nicotinic acid (I) with SOCl2 gives the corresponding acyl chloride (II), which is condensed with 2-methylpyrazolo[1,5-a]pyridine (III) by heating at 160-80 C or in refluxing dioxane, yielding 2-methyl-3-(3-pyridylcarbonyl)pyrazolo[1,5-a]pyridine (IV). Finally, this compound is hydrogenated with H2 over Pd/C in ethanol at 13 Atm. pressure and 55-8 C.
| 【1】 Hausberg, H.-H.; Koppe, V.; Poetsch, E.; Saiko, O.; Seyfried, C. (Merck Patent GmbH); Indolalkylamines, pharmaceutical compsns. containing them and process for their preparation. EP 0007399 . |
| 【2】 Castaner, J.; Prous, J.; KC-764. Drugs Fut 1991, 16, 2, 108. |
| 【3】 Awano, K.; Segawa, M.; Suzue, S.; Synthesis of 3-substituted pyrazolo[1,5-a]pyridine derivatives with inhibitory activity on platelet aggregation. I. Chem Pharm Bull 1986, 34, 7, 2828-32. |