158563-91-8Relevant academic research and scientific papers
Preparation method of 7-phenylindole compound
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Paragraph 0049; 0057-0059, (2020/11/01)
The invention discloses a preparation method of a 7-phenylindole compound. Indole is used as a starting raw material, under the condition that n-butyllithium is used as an alkali, a di-tert-butylphosphine guide group is introduced to the C1 site of an indole ring, a steric effect and a coordination effect are utilized to activate a carbon-hydrogen bond at the C7 site of the indole ring, and palladium acetate is adopted to catalyze an organic tin reagent to perform a carbon-carbon bond coupling reaction, so that arylation of the C7 site of the indole ring is realized; and by taking tetrabutylammonium fluoride as an alkaline condition, removing of the di-tert-butylphosphine guide group is carried out to obtain the 7-phenylindole compound. According to the method, halogenation does not need to be conducted at the C7 position of the indole ring in advance, the optimized reaction condition is mild, the substrate universality is good, the reaction yield is high, and the method is a new method for synthesizing the 7-phenylindole compound.
