| 盐酸阿那格雷的合成 |
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| 引用本文： | 翁志洁,李建其,周斌.盐酸阿那格雷的合成[J].中国医药工业杂志,2012,43(6):405-408. |
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| 作者姓名： | 翁志洁 李建其 周斌 |
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| 作者单位： | 中国医药工业研究总院上海医药工业研究院,创新药物与制药工艺国家重点实验室,上海200040 |
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| 摘 要： | 用间氯苯胺、水合氯醛和盐酸羟胺经缩合、环合、氯代及氧化反应制得6-氨基-2,3-二氯苯甲酸,再经环合、氯代、还原、取代、环合及成盐等反应制得抗凝血药盐酸阿那格雷,总收率约6.6％(以间氯苯胺计).
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| 关 键 词： | 盐酸阿那格雷 血小板增多症 合成 |
Synthesis of Anagrelide Hydrochloride |
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| Authors: | WENG Zhijie LI Jianqi ZHOU Bin |
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| Institution: | (State Key Lab.of New Drug and Pharmaceutical Process,Shanghai Institute of Pharmaceutical Industry,China State Institute of Pharmaceutical Industry,Shanghai 200040) |
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| Abstract: | Anagrelide hydrochloride,an antithrombotic drug,was synthesized from m-chloroaniline by condensation with chloral hydrate and hydroxylamine hydrochloride,and then through cyclization,chlorination and oxidation to give 6-amino-2,3-dichlorobenzoic acid(5),which was subjected to cyclization,chlorination,reduction,substitution,cyclization and salt formation with an overall yield of about 6.6%(based on m-chloroaniline). |
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| Keywords: | anagrelide hydrochloride essential thrombocytosis synthesis |
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