Preparation method of 6, 7-disubstituted-3-azabicyclo [3, 2, 1] octane derivative
The invention relates to a preparation method of a 6, 7-disubstituted-3-azabicyclo [3, 2, 1] octane derivative, and belongs to the field of organic synthesis. The preparation method comprises the following steps: constructing a bicyclic precursor 3 through Diels-Alder reaction, oxidizing a double bo...
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Zusammenfassung: | The invention relates to a preparation method of a 6, 7-disubstituted-3-azabicyclo [3, 2, 1] octane derivative, and belongs to the field of organic synthesis. The preparation method comprises the following steps: constructing a bicyclic precursor 3 through Diels-Alder reaction, oxidizing a double bond by potassium osmate to form a vicinal diol compound 4, performing oxidation reaction by sodium periodate to obtain dialdehyde 5, and finally performing reductive amination ring closing on the compound 5 and amine 6 to obtain the 6, 7-disubstituted-3-azabicyclo [3, 2, 1] octane derivative. The reaction route has the advantages that the used raw materials are easy to obtain, the atom economy is high, the reaction timeliness is high, the route is novel, the treatment is simple, and the production is easy.
本发明涉及一种6,7-二取代-3-氮杂二环[3,2,1]辛烷衍生物的制备方法,属于有机合成领域。该反应通过狄尔斯-阿尔德反应构建双环前体3,再通过双键被锇酸钾氧化形成邻二醇化合物4,后经高碘酸钠氧化反应得到二醛5,最后通过化合物5与胺6的还原胺化关环得到6,7-二取代-3-氮杂二环[3,2,1]辛烷衍生物。该反应路线优点在于所用原料易得,原子经济性高,反应时效性高,路线新颖,处理简单,易于生产。 |
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