盐酸沙格雷酯的合成 |
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引用本文: | 王振,杨秦亮.盐酸沙格雷酯的合成[J].广州化工,2014(8):52-53. |
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作者姓名: | 王振 杨秦亮 |
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作者单位: | [1]山东大学药学院,山东济南250012 [2]济南齐拓医药科技有限公司,山东济南250101 |
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摘 要: | 以2-((3-甲氧基)苯乙基)苯酚为起始物料,与环氧氯丙烷进行酚醚化反应得到2-2-(3-甲氧基)苯乙基]苯氧基]甲基]环氧乙烷,与二甲胺进行氨化反应得到1-二甲胺基-3-2-2-(3-甲氧基)苯乙基]苯氧基]-2-丙醇,再与丁二酸酐在有机溶剂中进行酯化反应得到沙格雷酯,最后通入氯化氢气体成盐即可制得盐酸沙格雷酯,总收率约67%。
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关 键 词: | 盐酸沙格雷酯 -HT受体拮抗剂 合成 |
The Synthesis of Sarpogrelate Hydrochloride |
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Affiliation: | WANG Zhen, YANG Qin -liang (1 School of Pharmacy, Shandong University, Shandong Jinan 250012; 2 Jinan Qituo Medical Scienee and Teehnology Co. , Ltd. , Shandong Jinan 250101, China) |
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Abstract: | Sarpogrelate Hydrochloride was synthesized from the 2 - (( 3 -methoxy ) phenylethyl ) phenol, etherification reaction of phenol with epichlorohydrin to 2 - 2 - ( 3 - methoxy) phenylethyl ] - phenoxy ] - methyl ] epoxyethane, ammonification reaction with dimethylamine to 1 - dimethylamine - 3 - 2 - 2 - (3 - methoxy ) phenylethyl] -phenoxy ] -methyl ] -2 -propoxyl, and then esterification reaction with Succinic anhydride to Sarpogrelate, acid salt can be obtained by organic solvent with an overall yield of about 67%. |
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Keywords: | Sarpogrelate Hydrochloride 5 - HT2 receptor - antagonist synthetic |
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