Synthesis method and application of 1, 3-aza-silane compound

Abstract

The invention discloses a synthesis method and application of 1, 3-aza-silane compounds, and belongs to the technical field of chemical synthesis of silicon nitrogen compounds. The inventor provides a novel synthesis method of a precursor compound 1, 3-aza-silane compound, and the precursor compound 1, 3-aza-silane compound is used as an initial raw material for preparing silicon-substituted indoline or other pharmaceutical compositions, so that the subsequent preparation method is easy to operate, low in related reagent risk, not harsh in reaction condition and the like, and further, the 1, 3-aza-silane compound is ensured to be high in yield. The 1, 3-aza-silane compound has strong applicability when being used as a reaction substrate, realizes the synthesis of silicon-substituted indoline, and provides reference precursor compound selection for new drug research and development and the like.

Description

technical field [0001] The invention relates to a method for synthesizing a class of 1,3-azasilane compounds and applications thereof, and belongs to the technical field of chemical synthesis of silicon-nitrogen compounds. Background technique [0002] 1,3-Azasilane compounds are a class of simple and efficient synthons for the construction of silazacyclic rings. In 2000, Voronkov's group reported that 1,3-azasilane compounds containing alkenyl or allyl silicon in Hg(OAc) 2 Under the catalysis, the nucleophilic attack of the nitrogen atom in the molecule to the unsaturated carbon atom at the β-position of the silicon group occurs in a cyclization reaction to generate silylpyrrolidine ( figure 1 ); in 2014, Maddauno's group reported that the ortho-linked 1,3-azasilane in bromobenzene was exchanged with lithium bromide to generate two forms of benzosilazane through sila-Matteson rearrangement. membered heterocycle ( figure 2 ); in 2018, Hartwig’s group reported that 1,3-az...

AI Technical Summary

Problems solved by technology

But these two kinds of methods all obtain the target product by prefabricating the reaction substrate containing silicon-nitrogen substitution to undergo an intramolecular cyclization reaction, and use harmful transition metal catalysts, which will cause problems such as environmental pollution; in addition, due to the need to The functional groups containing silicon and nitrogen are preformed on the substrate, which makes the synthesis of the substrate difficult and the scope of application is relatively limited.

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