53687-75-5Relevant academic research and scientific papers
Synthesis method of 2-aryl benzazepine and derivatives thereof
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Paragraph 0017; 0019-0027, (2021/11/14)
The invention relates to a synthesis method of 2-aryl benzazepine and derivatives thereof, the method comprises the following steps: stirring and reacting 2-halogenated aniline and aryl cyclobutanol as reaction substrates, palladium chloride as a catalyst, tricyclohexylphosphine as a ligand, cesium carbonate as alkali and ultra-dry toluene as a solvent in a nitrogen atmosphere at 110 DEG C for 12 hours. The method has the advantages of simple and easily available raw materials, relatively mild reaction conditions, wide substrate universality, novel preparation process, low energy consumption and the like.
Preparation method of polysubstituted benzo [b] azepine compound
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Paragraph 0019-0020, (2021/03/31)
The invention discloses a preparation method of a polysubstituted benzo [b] aza compound. According to the method, a series of polysubstituted benzo [b] aza-compounds are synthesized through aminationand intramolecular cyclization reactions of 1, 4-diarylalkyne and hydroxylamine trifluoromethanesulfonate. The method has the advantages of simple and accessible raw materials and mild reaction conditions, avoids the use of a transition metal catalyst, and is green and environment-friendly. Meanwhile, the method has the characteristics of good substrate compatibility, high yield, high atom economy and the like. The polysubstituted benzo [b] aza-compound is synthesized in one step by utilizing simple alkyne through a one-pot method, and a new path and a new method are provided for preparing anovel benzo [b] aza-compound with high pharmacological activity.
