Synthesis methods of 2, 5-dioxa-8-azaspiro [3.5] nonane and salt thereof

The invention discloses a synthetic method of 2, 5-dioxa-8-azaspiro [3.5] nonane. The method comprises the following steps: 1, reacting a compound 1 with chloroacetyl chloride in a first reaction solvent under the action of first alkali to obtain a compound 2; 2, carrying out self cyclization on the...

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Hauptverfasser: DONG JINGCHAO, YU LINGBO, TAN RUPENG, GAO MINGFEI, MAO YANJUN, MA RUJIAN, BAI YOUYIN, ZHAO TING, ZHOU QIANG, XU YAN, JIAO JIASHENG, XU XUEQIN, SUN CHUN, ZHANG DAWEI, LAN QIANQIAN, YAO BAOYUAN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a synthetic method of 2, 5-dioxa-8-azaspiro [3.5] nonane. The method comprises the following steps: 1, reacting a compound 1 with chloroacetyl chloride in a first reaction solvent under the action of first alkali to obtain a compound 2; 2, carrying out self cyclization on the compound 2 in an inert atmosphere in a second reaction solvent under the action of second alkali to generate a compound 3; 3, reducing the compound 3 by a reducing agent in a third reaction solvent in an inert atmosphere to obtain a compound 4; and 4, carrying out catalytic hydrogenation on the compound 4 to remove a Bn protecting group so as to obtain a compound 5. Compared with the prior art, the method provided by the invention has the advantages of easily available raw materials, short route, higher yield and easily controllable reaction, and is suitable for industrial production. 本发明公开了一种2,5-二氧杂-8-氮杂螺[3.5]壬烷的合成方法,包括如下步骤:第一步,以化合物1在第一反应溶剂中和氯乙酰氯在第一碱的作用下发生反应,得到化合物2;第二步,化合物2在惰性氛围、第二反应溶剂中,在第二碱的作用下发生自身环合生成化合物3;第三步,化