Synthesis method of tert-butyl-1, 7-diazaspiro [3.5] nonane-1-formate

The invention relates to a synthesis method of tert-butyl-1, 7-diazaspiro [3.5] nonane-1-formate, and mainly solves the technical problem that no suitable industrial synthesis method exists at present. The method comprises the following seven steps: 1, reacting a compound 1 with ethyl malonate added...

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Hauptverfasser: YU LINGBO, TAN RUPENG, GAO MINGFEI, WEI XINRUI, MA RUJIAN, FU XINYU, JIA TAO, BAI YOUYIN, ZHAO TING, ZHOU QIANG, SUN CHUN, ZHANG DAWEI, LAN QIANQIAN, YAO BAOYUAN, WANG XI, WEI WEI
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to a synthesis method of tert-butyl-1, 7-diazaspiro [3.5] nonane-1-formate, and mainly solves the technical problem that no suitable industrial synthesis method exists at present. The method comprises the following seven steps: 1, reacting a compound 1 with ethyl malonate added into a solvent ethanol to obtain a compound 2; 2, reacting the compound 2 with lithium borohydridein tetrahydrofuran to obtain a compound 3; 3, reacting the compound 3 with p-toluenesulfonyl chloride in dichloromethane to obtain a compound 4; 4, adding cesium carbonate into the compound 4 in acetonitrile serving as a solvent for cyclization to obtain a compound 5; 5, adding magnesium chips into the compound 5 in methanol serving as a solvent for reduction to obtain a compound 6, 6, reacting the compound 6 with Boc anhydride in dichloromethane to obtain a compound 7, and 7, reacting the compound 7 with palladium on carbon in methanol to obtain a final compound 8. 本发明涉及一种叔丁基-1,7-二氮杂螺[3.5]壬烷-1-甲酸基酯的合成方法,主要解决目前没有适合工业化