Scientists collide with the most difficult indulge association with copper, and open new drugs

Due to its properties, Indoles gained attention as an external column to collect a wide range of medicines. Since 2015, the US Food and Drug Administration has approved 14 endophood drugs to treat cases, such as migraines, infections and high blood pressure. Chemists have developed many strategies to connect different chemical groups to indhes. Some methods offer new groups directly on the episode, while others include temporary structural changes through mediators. However, modifying specific places on the endopolis loop, such as C5 Carbon, still represents a challenge due to its low interaction.

In a recent study, researchers at the University of Chiba, Japan, reported a method to selectively connect the Alkeil group to the C5 from the Andol using a relatively inexpensive copper catalyst, which produced the desired product in a yield of up to 91 %. This method provides a more affordable and developed approach to Indoor modification, which can be of special value in the development of medicines.

The study included, led by Assistant Professor Shingo Harada, Mr. Tomohiro Isono, B. Farm. , Mrs. May Yanagawa, M. , Professor Titsuhiro Nemoto of the College of Graduate Studies for Pharmaceutical Sciences at the University of Chiba, and was published on the Internet in the magazine on the Internet in the magazine Chemical sciences.

“We have developed the direct and selective C5-H functional reaction of the indol for copper stimulus. The resulting compounds contain common structural features in natural endopolis alkaloids and drug molecules, highlighting the benefit of this approach to making important compounds biologically,” says Dr. Hararada.

Carbine reaction, and high -reactionary carbon species that can form new carbon bonds. In a previous study, the Rhodium -based carbon team used to connect groups in the C4 position of indol, guiding the unprotected Enone groups placed in place 3. In this study, they used a similar strategy but changed the conditions of interaction to target the C5 position instead.

Test the reaction using the model compound, N-Benzyl Indole with the ENONE group, along with the α-diazomalonates α-diazomalonates as a source of carbine and different groups of copper, copper and silver salts as buses. Initially, the desired product C5 function was formed only in small quantities, with returns up to 18 %. However, when they used a set of copper and silver salts (CU (OAC)₂H₂Q and AGSBF₆The return rose to 62 %. When making more improvements, such as setting the size of the solvent and increasing the concentration, they improved the return to 77 %.

The reaction has proven that it is very versatile, and works with a wide range of Andoli. When the Enone group was replaced in Place 3 with the benzwell group, the return increased to 91 %. Successful reactions have also been observed with Ando bearing other alternatives, such as Metoxiple, allers, and Vinyl, and opened the door to the creation of various structural molecules.

To detect the interaction mechanism, the team made quantitative chemical calculations, indicating that carbine does not interact directly in the C5. Instead, it first forms a bond in the C4 position, creating a tense loop of three members. Then this means rearrange, and convert the new bond to the C5 position. The copper catalyst plays an important role in making this path possible by installing the broker and lowering the power barrier to rearrange.

This copper stimulating strategy provides a reliable and cost -effective approach to the modification of the Andoli in the position of C5, which results in compounds that are closely similar to the factors based on biologically active and active. Dr. Harrada highlights the possibilities of the method to discover drugs by saying, “While it may not cause a major shift immediately, it may enhance continuous progress in the discovery of drugs, which leads to a small long -term effect.”

The team continues its research, and exploring other carbonics reactions to develop more selective and effective strategies to create molecules based on Andol that may one day contribute to the treatment of specific diseases.