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The Development of Tolvaptan Manufacturing Process:Unexpected Solvent Effect on Acylation Reaction with AcidChloride

机译：托勒瓦班制造过程的发展：与酸氯化物酰化反应的意外溶剂效应

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Tolvaptan is a non-peptide arginine vasopressin V2 receptor antagonist,which is usedfor treatment of hyponatremia.Structurally,tolvaptan is an acylated5-hydroxy-2,3,4,5-tetrahydro-1H-benzoazepine.The coupling between the5-hydroxy-2,3,4,5-tetrahydro-1H-benzoazepine and the corresponding acid chloride withoutprotection of the benzyl alcohol is an attractive manufacturing method for tolvaptan.Wehave successfully developed the manufacturing method for tolvaptan by amidation within-situ prepared acid chloride solution without removing excess amount of thionyl chloride.

机译：Tolvaptan是一种非肽精氨酸血管加压素V2受体拮抗剂，用于治疗低钠血症。结构，托尔瓦替丹是酰化5-羟基-2,3,4,5-四氢-1H-苯并杂志。5-Hydroxy-2之间的偶联，3,4,5-四氢-1H-苯并嗪和相应的酰氯的酰氯是苄醇的耐受性制造方法.Wehave通过酰胺化在原位内制备的酰氯溶液而成功地开发了托尔瓦夫坦的制造方法，而不会除去过量亚硫酰氯的量。

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《日本化学会春季年会》|2020年|1 CD-ROM|共1页
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作者
Hideyuki Sogo; NaokiOno; Junpei Sukegawa;
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中图分类石油化学工业;
关键词
Amide; Active pharmaceutical ingredients; Acid chloride; Solvent effect;

机译：酰胺;活性药物成分;酰氯;溶剂效果;

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4. The Development of Tolvaptan Manufacturing Process:Unexpected Solvent Effect on Acylation Reaction with AcidChloride [C] . Hideyuki Sogo, NaokiOno, Junpei Sukegawa 日本化学会春季年会 . 2020

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The Development of Tolvaptan Manufacturing Process:Unexpected Solvent Effect on Acylation Reaction with AcidChloride

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