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治疗帕金森氏病常用药物有左旋多巴或左旋多巴/卡比多巴的复合制剂,由于左旋多巴疗效低以及存在急、慢性副作用,使其使用受到限制。现已研究了多巴胺激动剂作为治疗帕金森氏病的替代药,近年在临床应用的三个多巴胺激动剂是:溴隐亭、lisuride hydrogen meleate和pergo1ide mesy1ate。后者是今年上市的。正在美国进行临床评价的另三个多巴胺激动剂是:N-0437、Talipexole.2HC1和Naxagolide.HCl。合成本品可通过三种不同途径获得: 1.2-氨基-7-甲氧基-1-四氢萘酮(Ⅰ)用氯乙酰氯酰化得Ⅱ,Ⅱ用NaBH_4还原成Ⅲ,Ⅲ通过NaH环合成Ⅳ,用LiAH_4将Ⅳ回
Drugs commonly used in the treatment of Parkinson’s disease with levodopa or levodopa / carbidopa compound preparation, due to the low efficacy of levodopa and the presence of acute and chronic side effects, its use is limited. Dopamine agonists have been studied as surrogate drugs for the treatment of Parkinson’s disease. Three dopamine agonists for clinical use in recent years are: bromocriptine, lisuride hydrogen meleate and pergo1ide mesy1ate. The latter is listed this year. Three other dopamine agonists currently under clinical evaluation in the United States are: N-0437, Talipexole. 2HC1 and Naxagolide.HCl. The synthesis of this product can be obtained by three different routes: 1.2-amino-7-methoxy-1-tetralone (Ⅰ) acylation with chloroacetyl chloride Ⅱ, Ⅱ with NaBH_4 reduction Ⅲ, Ⅲ by NaH Synthesis Ⅳ, with LiAH_4 IV back