Synthetic method of pyrrol-indole compound as drug intermediate

Abstract

The invention relates to a synthetic method of a pyrrol-indole compound shown in the formula (IV) (in the description). The method comprises the following steps: in a room-temperature and nitrogen environment, sequentially adding a compound shown in the formula (I) (in the description), a compound shown in the formula (II) (in the description), a compound shown in the formula (III) (in the description), a composite catalyst, gallium trichloride and organic alkali into an organic solvent, then, heating to 70-85 DEG C, performing full stirring reaction for 4-6 hours at the temperature of 70-85 DEG C, and performing postprocessing, so as to obtain the compound shown in the formula (IV), wherein in the formulas, R1 is selected from H or C1-C6 alkyl groups; R2 is selected from H, C1-C6 alkyl groups, C1-C6 alkoxy groups or halogen; A is substituted and unsubstituted C5-C8 naphthenic bases, or substituted and unsubstituted phenyl groups. According to the method, the appropriate reaction substrates, the catalyst, the organic alkali and the organic solvent are comprehensively selected and coordinated, and the gallium trichloride is used, so that the target product can be obtained with high yield, and the method has good application prospect and high market popularization value in the field of synthesis of medical intermediates.

Description

technical field [0001] The invention relates to a method for synthesizing condensed ring compounds, more specifically to a method for synthesizing pyrroloindole compounds, and belongs to the field of synthesizing pharmaceutical intermediates. Background technique [0002] In the fields of medicine, medical treatment, organic synthesis, etc., natural products containing indole structures occupy a very important position, because the structures containing indole often show good biological activities. Among the indole compounds, the pyrroloindole compounds are more important, which exist in a large number of alkaloids as the parent skeleton. [0003] It is precisely because of the important role of pyrroloindole compounds that the development of new synthetic techniques for pyrroloindole compounds will facilitate the synthesis of drugs and their intermediates. [0004] In recent years, a variety of synthetic methods for indole skeleton structures have been developed in the pri...

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Problems solved by technology

[0009] As mentioned above, various synthesis methods of pyrroloindole compounds have been disclosed in the prior art. However, these methods have many defects, such as a narrow range of substrates, the need for pre-functional modification of starting materials, the use of Highly toxic reagents, etc., these problems will inevitably affect the efficiency and safety of industrial scale-up production

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