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噻氯匹定

噻氯匹定

CAS号:55142-85-3
英文名:ticlopidine
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化合物简介
Ticlopidine (trade name Ticlid) is an antiplatelet drug in the thienopyridine family which is an adenosine diphosphate (ADP) receptor inhibitor. Research initially showed that it was useful for preventing strokes and coronary stent occlusions. However, because of its rare but serious side effects of neutropenia and thrombotic thrombocytopenic purpura it was primarily used in patients in whom aspirin was not tolerated, or in whom dual antiplatelet therapy was desirable. With the advent of newer and safer antiplatelet drugs such as clopidogrel and ticagrelor, its use remained limited.
基本信息
编号系统
安全信息
生产方法及用途
生产方法
噻吩溶于无水乙醚,在0℃缓慢滴加丁基锂乙醚溶液,再在室温搅拌。然后滴加环氧乙烷乙醚溶液,处理得2-羟乙基噻吩。将其溶于吡啶,在5℃以下分批加入对甲苯磺酰氯,室温搅拌,处理得磺酰化产物。该磺酰化产物和邻氯苄胺溶于甲苯,回流。滤除固体,滤液用盐酸提取。提取液浓缩,放置。沉淀用丙酮洗。然后将其与甲醛及水搅拌,回流,滤液用稀氢氧化钠碱化,异丙醚提取,经处理加入少许浓盐酸和丙酮,放置,析出结晶,即为盐酸噻氯匹定。
用途
抗血小板聚集药,能抑制ADP、胶原、凝血酶、花生四烯酸以及前列腺素内过氧化物等多种诱导剂引起的血小板聚集,能抑制外源和内源性ADP诱导的血小板聚集反应。用于血管手术和体外循环发生的血栓、动脉闭塞性脉管炎及闭塞性动脉硬化。可降低中风、心肌梗死或血栓栓塞性卒中的血管坏死发生率。