The Oxidative Activation Reaction Of The Carbon-hydrogen Bond's Functionalization Of 4H-?-Carboline Compounds By TEMPOBF4 And Extend With Various Nuclear Reagents

Purpose of Research: In recent years, the field of hydrocarbon activation concern. Through a series of literature study, we found that now most of the activation process requires participation of organometallic reagents for hydrocarbon activation, and reaction conditions are relatively harsh. In this paper, a simple hydrocarbon activation exposition, and through the course of the study cited in recent years related to group in the article to illustrate different functional activation of carbon-hydrogen bonds, and according to the relevant survey proposed research purpose of this subject, namely on the basis of previous work, which does not require metal to build participation, non-polluting, efficient, less by-products, economical and environmentally friendly method of activation and common hydrocarbon raw materials, in order to further facilitate the production and application.Methods of Research: The subject was monitored by TLC using a variety of methods, mass spectrometry and NMR studies to expand through a series of preliminary experiments and investigations, and screened many similar drugs 4H-?- carboline structure as substrate the experiment, whereby explore TEMPO oxidative coupling system without the participation of the metal directly contribute to the possibility of oxidative coupling; and the reaction temperature, the reagents and other aspects of the equivalent filter optimization. Optimum reaction conditions: an oxidant TEMPOBF4(0.20 mmol, 1.00 eq), a solvent of DCM(2.00 mL), phenylacetylene nucleophile BF3 ? K(0.40 mmol, 2.00 eq). Under the premise of optimal reaction conditions, the structure of the relevant type nucleophile extended, were selected to different BF3 ? K salt as nucleophile experiment.Research findings: In this subject,the needs of catalytic oxidation of metal-free condition is extremely gentle and simple, environmentally friendly, low cost, high oxidation resistance and other characteristics,and by the good oxidation of TEMPOBF4, established a new oxide coupling system for catalytic oxidation and extends the range ofthe nucleophile, experiments show that the expansion of the nucleophile can be well adapted to the conditions, and oxidative coupling product obtained with a higher yield..Conclusion: TEMPOBF4 oxidative coupling system is more widely for different BF3 ? K nucleophiles, such as reaction with BF3 ? K of phenylacetylene and styrene as well as heterocyclic and other nucleophiles: the simple experiment operation, mild reaction conditions, in line with the principle of atom economy, which provides a new way for the synthesis of natural products and drugs.