| 王金朋,王诗玺,刘世旭,等.以天冬氨酸和丙氨酸为起始原料合成2-甲基-3-羟基吡啶[J].中国海洋药物,2018,37(5):74-78. |
| 以天冬氨酸和丙氨酸为起始原料合成2-甲基-3-羟基吡啶 |
| The synthesis of 3-hydroxyl-2-methylpyridine by aspartic acid and alanine as starting material |
| 投稿时间：2018-03-29 修订日期：2018-05-11 |
| DOI： |
| 中文关键词: 丙氨酸 天冬氨酸 2-甲基-3-羟基吡啶 噁唑环 Diels-Alder反应 |
| English Keywords:alanine aspartic acid 3-hydroxyl-2-methylpyridine oxazole ring Diels-Alder reaction |
| Fund Project: |
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| 中文摘要: |
| 目的 获得2-甲基-3-羟基吡啶合成方法，降低2-甲基-3-羟基吡啶的合成成本，为常山酮等药物的合成提供了廉价原料。方法 分别以天冬氨酸和丙氨酸为起始原料，经过噁唑中间体，利用Diels-Alder反应，最后脱羧获得2-甲基-3-羟基吡啶，总收率7.4%和30.3%。结果 提供了1种合成2-甲基-3-羟基吡啶的方法，丙氨酸为原料的方法更适合工业化生产，且合成方法简单、原料价格低廉，极大降低了2-甲基-3-羟基吡啶的合成成本，为常山酮等药物的合成提供了廉价原料。 |
| English Summary: |
| Objective To obtain the synthetic methods of 3-hydroxyl-2-methylpyridine, decrease synthetic costs and provide cheap intermediate for synthesis of halofuginone and other drugs. Methods In the study, we explored and obtained two synthetic methods having total yield of 7.4% and 30.3% for 3-hydroxyl-2-methylpyridine by aspartic acid and alanine as starting material respectively. The product was given through two methods, in which the formation of oxazole ring intermediate, Diels-Alder reaction and decarboxylation were carried out in sequence. Results The synthetic method by alanine as starting material was more suitable for the industry production because of the cheap starting material, higher yield, lower synthetic costs and finally provided cheap intermediate for synthesis of halofuginone and other drugs. |
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