| 6-甲基-4-羟基-噻嗯并[2,3-b]噻喃-2-磺酰胺的合成 |
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| 引用本文： | 江曦,杨艺虹,张珩,杨建设,刘磊.6-甲基-4-羟基-噻嗯并[2,3-b]噻喃-2-磺酰胺的合成[J].应用化工,2007,36(12):1215-1217. |
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| 作者姓名： | 江曦 杨艺虹 张珩 杨建设 刘磊 |
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| 作者单位： | 武汉工程大学,湖北省新型反应器与绿色化学工艺重点实验室,湖北,武汉,430073 |
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| 摘 要： | 以2-巯基噻吩和巴豆酸为起始原料,经加成缩合制得3-(2-噻吩巯基)丁酸;在P2O5催化下环合制得6-甲基-4-氧-噻嗯并2,3-b]噻喃;再用氯磺酸进行氯磺化、氨水氨解制得6-甲基-4-氧-噻嗯并2,3-b]噻喃-2-磺酰胺;最后用硼氢化钠还原得到盐酸杜塞酰胺的中间体6-甲基-4-羟基-噻嗯并2,3-b]噻喃-2-磺酰胺,合成总收率为16.0%。其化学结构经IR,1H NMR,MS得以确证。
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| 关 键 词： | 6-甲基-4-羟基-噻嗯并噻喃-2-磺酰胺 中间体 盐酸杜塞酰胺 合成 |
| 文章编号： | 1671-3206（2007）12-1215-03 |
| 收稿时间： | 2007-09-28 |
| 修稿时间： | 2007年9月28日 |
Synthesis of 4-hydroxy-6-methylthieno[2,3-b]thiopyran-2-sulfonamide |
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| JIANG Xi,YANG Yi-hong,ZHANG Heng,YANG Jian-she,LIU Lei.Synthesis of 4-hydroxy-6-methylthieno[2,3-b]thiopyran-2-sulfonamide[J].Applied chemical industry,2007,36(12):1215-1217. |
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| Authors: | JIANG Xi YANG Yi-hong ZHANG Heng YANG Jian-she LIU Lei |
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| Abstract: | 4-Hydroxy-6-methylthieno2,3-b] thiopyran-2-sulfonamide,a intermediate of dorzolamide hydrochloride was synthesized from 2-mercaptothiophene and crotonic acid.Through addition to 3-(2-mercaptothiophene)butanoic acid.Through cycloration by phosphorus pentoxide,5,6-dihydro-6-methyl-4H-thieno2,3-b] thiopyrane-4-one was prepared.Through chlorosulfonylation by chlorosulfonic acid and amination by ammonium hydroxide,finally,5,6-dihydro-6-methyl-4H-thieno2,3-b] thiopyrane-4-one-2-sulfonamide was produced.Sodium borohydride,its overall yield was 16.0%.The chemical structure was confirmed by IR,1H NMR,MS. |
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| Keywords: | 4-hydroxy-6-methylthieno-thiopyran-2-sulfonamide intermediate dorzolamide hydrochloride synthesis |
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