Synthetic method of polysubstituted imidazoles

Abstract

The invention discloses a synthetic method of polysubstituted imidazoles, which is characterized in that, the method comprises the following steps: mixing acetophenone and benzylamine according to 1:3 proportion; stirring the mixture under the oxygen and solvent-free condition at 40 DEG C. and reacting for 24 hours; carrying out TLC detection; obtaining the object products by column chromatography isolation. The method does not need extra solvents, thereby reducing usage and discharge of organic solvent; the initial raw materials are cheap and easily available, and the synthesis cost is saved; the conversion of the reaction can be realized under the cuprous iodide and oxygen catalysis condition, and the catalysis condition is simple; the invention is carried out at 40 DEG C., and the reaction temperature low and the reaction condition is mild.

Description

Technical field [0001] The present invention is an organic chemistry and pharmaceutical chemistry field, and it involves a synthetic method of multi -alidazole. Background technique [0002] Multi -replacement of imidazole is an important type of nitrogen miscellaneous ring organic compound. Its skeleton exists in some natural products, drug molecules, functional polymer materials and organic synthetic intermediates. [0003] Idazole -type compounds are widely used in biomedical and are widely used, for example: [0004] cimetidine (1) (Anti -digestive ulcer); [0005] Ketoconazole (2) (antifungal medicine, Wilson and GISVOLD ’s Textbook of Organic Medicinal and Pharmaceutical Chemistry , 10th Ed.; Delgado, J. N., REMERS, W. A., EDS.; Lippincott-raven: Philadelphia, PA, 1998.); [0006] Apoptozle (3) (Treatment of cystic fiber, J. am. Chem. SoC. 2011, 133 , 2026-20276.). [0007] Judging from the current literature, the most commonly used method is: [0008] (1) 1,2-dione, al...

AI Technical Summary

Problems solved by technology

[0014] 1. Need to use strong acid or strong base, and some reaction temperature is relatively high;

[0015] 2. There are few reports on the synthesis methods of 1,2,4-multi-substituted imidazoles;

[0016] 3. The reaction substrate is difficult to prepare;

[0017] 4. The catalytic system needs to add an additional organic solvent;

[0018] 5. Some catalysts are toxic;

[0019] 6. Generate more by-products or lower yield

[0020] These disadvantages limit its application in synthetic

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