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| 盐酸替罗非班的合成 | |
| 引用本文： | 郑永勇,张子学,黄雷,李建其,周斌. 盐酸替罗非班的合成[J]. 中国医药工业杂志, 2012, 43(6): 408-410 |
| 作者姓名： | 郑永勇 张子学 黄雷 李建其 周斌 |
| 作者单位： | 中国医药工业研究总院上海医药工业研究院,上海药物合成工艺过程工程技术研究中心,上海200437 |
| 摘 要： | L-酪氨酸经三甲基硅烷基保护、磺酰化及脱保护制得N-(丁磺酰基)-L-酪氨酸(5),5与4-(4-氯丁基)吡啶盐酸盐经缩合、钯炭催化加氢及成盐反应制得血小板凝集抑制剂盐酸替罗非班,总收率约60%(以L-酪氨酸计)。 |
| 关 键 词： | 盐酸替罗非班 GPIIb/IIIa受体拮抗剂 血小板凝集抑制剂 合成 |
Synthesis of Tirofiban Hydrochloride |
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| ZHENG Yongyong , ZHANG Zixue , HUANG Lei , LI Jianqi , ZHOU Bin. Synthesis of Tirofiban Hydrochloride[J]. , 2012, 43(6): 408-410 | |
| Authors: | ZHENG Yongyong ZHANG Zixue HUANG Lei LI Jianqi ZHOU Bin |
| Affiliation: | (Shanghai Engineering Research Center of Pharmaceutical Process,Shanghai Institute of Pharmaceutical Industry,China State Institute of Pharmaceutical Industry,Shanghai 200437) |
| Abstract: | N-(Butylsulfonyl)-L-tyrosine(5) was synthesized from L-tyrosine by silylation with trimethylsilyl chloride,sulfonylation and deprotection.Compound 5 was condensed with 4-(4-chlorobutyl)pyridine hydrochloride,catalytic hydrogenation with Pd/C and salt formation to provide tirofiban hydrochloride.The overall yield was about 60%(based on L-tyrosine). |
| Keywords: | tirofiban hydrochloride glycoprotein Ⅱb/Ⅲa receptor antagonist platelet aggregation inhibitor synthesis |
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