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Aryne-based substituted indolizine derivative and preparation method and applications thereof

An indolazine and arylalkynyl technology, which is applied in the field of organic compound intermediate preparation, can solve problems such as few indolazine synthesis methods, and achieve the effects of low production cost, good reaction selectivity and mild reaction conditions

Inactive Publication Date: 2013-03-20
SHAOXING UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are few synthetic methods of indolezine reported so far

Method used

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  • Aryne-based substituted indolizine derivative and preparation method and applications thereof
  • Aryne-based substituted indolizine derivative and preparation method and applications thereof
  • Aryne-based substituted indolizine derivative and preparation method and applications thereof

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Embodiment 1～5

[0023] According to the raw material ratio in Table 1, weigh indolezine compound (II), 2,2-dibromovinyl aromatic compound (III), inorganic base, metal palladium catalyst and 2ml of N,N dimethylformamide (DMF) in a 25ml round-bottomed flask, under the protection of a nitrogen balloon, the reaction was completed according to the reaction conditions in Table 2, and then the solvent was spin-dried, and the obtained crude product was subjected to column chromatography (petroleum ether / ethyl acetate=10 / 1 ) purification to obtain the final product, the reaction results are shown in Table 2, and the reaction process is shown in the following formula:

[0024]

[0025] Table 1

[0026]

[0027] Table 2

[0028]

[0029] Wherein: Et is ethyl, n Bu is n-butyl, T is the reaction temperature, t is the reaction time, Et is ethyl, and Ph is phenyl.

[0030] Structure confirmation data:

[0031] The structural detection data of the aralkynyl-substituted indolezine derivatives pre...

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PUM

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Abstract

The invention discloses an aryne-based substituted indolizine derivative and a preparation method and applications thereof. The preparation method is characterized by comprising the following steps: under the condition of stirring, adding indolizine compounds, 2, 2-ethylene dibromide aromatic compounds, inorganic alkali and a metallic palladium catalyst into N, N-dimethyl formamide; and under the protection of nitrogen, carrying out complete reaction on the obtained mixture at a temperature of 80-100 DEG C, and carrying out post-treatment on the obtained product so as to obtain the aryne-based substituted indolizine derivative. According to the aryne-based substituted indolizine derivative and the preparation method, the aryne-based substituted indolizine derivative is prepared by using easily-available raw materials, the reaction selectivity is good, the reaction conditions are mild, the preparation process is simple, and the production cost is low.

Description

Technical field: [0001] The invention relates to the field of preparation of organic compound intermediates, in particular to an aralkynyl-substituted indolezine derivative, a preparation method and application thereof. Background technique: [0002] Indoxazine structural units widely exist in biologically active natural products and synthetic drugs. Therefore, how to synthesize indoxazine derivatives quickly, efficiently and greenly is of great significance. However, few synthetic methods of indoxazines have been reported so far. [0003] In recent years, the use of metal palladium to catalyze organic transformation processes has made great progress. Palladium as a catalyst to catalyze the synthesis of pharmaceutical intermediates has attracted worldwide attention. Using palladium catalysts to develop new synthetic processes for many pharmaceutical intermediates has good economic benefits, environmental benefits and industrialization prospects, and is expected to be appl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04A61P35/00
Inventor 赵保丽程凯胡六江
Owner SHAOXING UNIVERSITY
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