A Direct Approach to Decoration of Bioactive Compounds via C-H Amination Reaction
Guodong Ju1, Chunchen Yuan1, Dongjie Wang1
1Key Laboratory of Organic Synthesis of Jiangsu Province, College of Chemistry , Chemical Engineering and Materials Science Soochow University , Suzhou 215123 , P. R. China.
Abstract:
The development of new methods to achieve the direct synthesis of bioactive organic molecules is always an important topic in organic synthesis. We hereby demonstrate that N-methoxyamide is an excellent amino source in the iridium-catalyzed intermolecular C-H amination reaction. The linkage of two bioactive organic molecules can be well achieved with this new protocol. More than 20 examples of decorated bioactive compounds were reported, which can facilitate the discovery of new bioactive molecules.
Related Concept Videos
Preparation of 1° Amines: Hofmann and Curtius Rearrangement Mechanism
Amines to Amides: Acylation of Amines
Next, the second equivalent of amine serves as a Brønsted base and deprotonates the quaternary...
Preparation of 1° Amines: Gabriel Synthesis
Strong bases like NaOH or KOH deprotonate the phthalimide to form the corresponding anion, which acts as a nucleophile. Further, the anion attacks an...
Preparation of Amides
The DCC-promoted synthesis of amides begins with the protonation of DCC by carboxylic acid. The protonation makes it a better acceptor. Next, the addition of carboxylate to the protonated carbodiimide gives a reactive acylating agent.
Subsequently, the amine acts as a nucleophile that attacks the acylating agent to form a tetrahedral intermediate. In the...
Preparation of 1° Amines: Hofmann and Curtius Rearrangement Overview
Preparation of Amines: Reductive Amination of Aldehydes and Ketones


