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发明授权
CN101462986B (R)-5-(2-氨基丙基)-2-甲氧基苯磺酰胺的合成方法 失效 - 权利终止 转让

(R)-5-(2-氨基丙基)-2-甲氧基苯磺酰胺的合成方法
摘要：
本发明涉及(R)-5-(2-氨基丙基)-2-甲氧基苯磺酰胺的合成方法。该方法以对卤茴香醚为起始原料，通过和金属作用，对手性环氧丙烷或手性环氧氯丙烷开环的反应为关键反应，将新生成的羟基和取代的苯磺酰氯或甲磺酰氯反应做成离去基团，然后经过氨解或叠氮化，水解或还原为胺，保护氨基，苯环磺化，酰化，胺解，脱氨基保护，得到(R)-5-(2-氨基丙基)-2-甲氧基苯磺酰胺。
摘要（英）：

The invention relates to a method for synthesizing (R)-5-(2-aminopropyl)-2-methoxyl benzsulfamide. In the method, dihalogen anisole is used as initial raw material to react with metal. The reaction for opening ring of chiral propylene oxide or chiral epoxy chloropropane is the key reaction. Newly generated hydroxide radical reacts with substituted benzene sulfone chloride or methylsulfonyl chloride to generate leaving group to be ammonolyzed or azided and hydrolyzed or reduced into amine. (R)-5-(2-aminopropyl)-2-methoxyl benzsulfamide is prepared by protecting amido, benzene ring sulfonation,acylatation, aminolysis and deamination protection.

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