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托伐普坦的合成 被引量：7

Synthesis of Tolvaptan
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摘要 7-氯-5-氧代-2,3,4,5-四氢-1H-苯氮(?)经酰化、还原得到1-(4-氨基-2-甲基苯甲酰基)-7-氯-5-氧代-2,3,4,5-四氢-1H-1-苯氮(?),再经邻甲基苯甲酰氯酰化、硼氢化钠还原制得选择性精氨酸加压素V_2受体拮抗剂托伐普坦,总收率约45%。 Tolvaptan,a selective nonpeptide arginine vasopressin V_2 receptor antagonist,was synthesized from 7-chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine by acylation and reduction to give 1-（4-amino-2-methylbenzoyl） -7- chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine,which was subjected to acylation with 2-methylbenzoyl chloride and reduction with sodium borohydride with an overall yield of about 45%.
作者 杨传伟 穆帅 刘颖 王平保 刘登科
机构地区 河南大学药学院 天津大学化工学院 天津药物研究院
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2011年第2期90-92,共3页 Chinese Journal of Pharmaceuticals
基金 天津市科技计划项目(09ZCKFSH01300)
关键词 托伐普坦 精氨酸加压素V_2受体拮抗剂 心衰 低钠血症 合成 tolvaptan arginine vasopressin V_2 receptor antagonist heart failure hyponatremia synthesis
分类号 R972.1 [医药卫生—药品]
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二级参考文献13

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共引文献9

同被引文献60

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  • 6Gheorghiade M, Konstam M A, Burnett J C, et al. For the effecacy of vasopressln antagonism in heart failure: Outcome study with tolvaptan(EVEREST) investigators [ J]. J Am Med Assoc,2007,297 : 1332 - 1343.
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  • 10Ghali JK, Zmily HD, Farah JO, et al. Lixivaptan, a non- peptide vasopressin V2 receptor antagonist for the potential oral treatment of hyponatremia [J]. IDrugs, 2010, 13 (11): 782-792.

引证文献7

二级引证文献11

中国医药工业杂志
2011年 第2期

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