| 盐酸吡格列酮的合成新方法研究 |
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| 引用本文： | 杨可锋,戴立言,陈英奇.盐酸吡格列酮的合成新方法研究[J].有机化学,2004,24(8):890-892. |
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| 作者姓名： | 杨可锋 戴立言 陈英奇 |
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| 作者单位： | 1. 浙江大学材料与化工学院制药工程研究所,杭州,310027;浙江华义医药有限公司,义乌,322002
2. 浙江大学材料与化工学院制药工程研究所,杭州,310027 |
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| 摘 要： | 报道了治疗糖尿病药物盐酸吡格列酮的合成新方法.在六氢吡啶作用下,对羟基苯甲醛和2,4-噻唑烷二酮缩合生成5-(4-羟苯基)亚甲基]-2,4-噻唑烷二酮,经钯炭催化氢化还原生成5-(4-羟苯基)甲基]-2,4-噻唑烷二酮,再和氢氧化钾反应生成相应的钾盐,然后与5-乙基-2-羟乙基吡啶和甲基磺酰氯反应得到的磺酸酯作用生成吡格列酮,最后用盐酸酸化得到其盐酸盐.产品结构经1H NMR和IR确证.
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| 关 键 词： | 盐酸吡格列酮 合成 新方法 |
| 修稿时间： | 2003年10月8日 |
New Synthetic Method of Pioglitazone Hydrochloride |
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| Abstract: | A new synthetic method of pioglitazone hydrochloride, a kind of drug for treating diabetes, was reported. With the piperidine as catalyst, p-hydroxybenzaldehyde condensed with 2,4-thiazolidinedione to give 5-(4- hydroxybenzylidene)thiazolidine-2,4-dione, which was reduced by hydrogen/Pd-C to afford 5-(4-hydroxybenzyl)~thiazolidine- 2,4-dione. The dione subsequently reacted with potassium hydroxide and 2-(5-ethyl-2-pyridyl)ethyl sulfonate to produce pioglitazone, and finally with hydrochloride acid to obtain the hydrochloride salt. Some compounds were confirmed by 1H NMR and IR. |
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| Keywords: | pioglitazone hydrochloride synthesis new method |
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