- Preparation method for 5-bromo-7-azindole
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The invention belongs to the technical field of preparation of 5-bromo-7-azindole, in particular to a preparation method for the 5-bromo-7-azindole. The method comprises the following steps: taking 2-amino-5-bromopyridine as a raw material, and performing the steps in sequence: (1) introducing iodine through an iodine reagent; (2) performing a coupling reaction with methylbutynol; and (3) performing a ring-closing reaction under the catalysis of inorganic strong base to prepare the 5-bromo-7-azindole, wherein the catalyst adopted in the coupling reaction in the step (2) is bis(benzonitrile)palladium dichloride or [1,1'-bis(diphenylphosphine)ferrocene]palladium dichloromethane dichloride complex compound. According to the preparation method, cheap 2-amino-5-bromopyridine is taken as the rawmaterial in the step (1); the catalyst with high catalyzing efficiency and a solvent which is easy to treat are adopted; purifying steps in each step are simple; the yield is high; and the and the yield of the finally prepared product, namely, the 5-bromo-7-azindole, can reach over 93 percent.
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- PROCESS FOR THE MANUFACTURE OF PHARMACEUTICALLY ACTIVE COMPOUNDS
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According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as novel synthesis routes for key intermediates used in those processes.
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Page/Page column 11-12
(2011/02/25)
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