27185-23-5Relevant academic research and scientific papers
Design, synthesis and characterization of novel N-heterocyclic-1-benzyl-1H-benzo[d]imidazole-2-amines as selective TRPC5 inhibitors leading to the identification of the selective compound, AC1903
Sharma, Swagat H.,Pablo, Juan Lorenzo,Montesinos, Monica Suarez,Greka, Anna,Hopkins, Corey R.
, p. 155 - 159 (2018/12/11)
The transient receptor potential cation channel 5 (TRPC5) has been previously shown to affect podocyte survival in the kidney. As such, inhibitors of TRPC5 are interesting candidates for the treatment of chronic kidney disease (CKD). Herein, we report the synthesis and biological characterization of a series of N-heterocyclic-1-benzyl-1H-benzo[d]imidazole-2-amines as selective TRPC5 inhibitors. Work reported here evaluates the benzimidazole scaffold and substituents resulting in the discovery of AC1903, a TRPC5 inhibitor that is active in multiple animal models of CKD.
Regioselective N-alkylation of 2-aminoimidazoles with alcohols to 2-(N-Alkylamino)imidazoles catalyzed by the [Cp*IrCl2] 2/K2CO3 system
Li, Feng,Kang, Qikai,Shan, Haixia,Chen, Lin,Xie, Jianjiang
, p. 5085 - 5092 (2012/11/13)
The direct N-alkylation of 2-aminoimidazoles to give the corresponding 2-(N-alkylamino)imidazoles was accomplished using alcohols as alkylating agents in the presence of a [Cp*IrCl2]2/K 2CO3 system. The iridium-catalyzed regioselective reaction is simple, efficient, general, and environmentally benign. The direct N-alkylation of 2-aminoimidazoles to give the corresponding 2-(N-alkylamino) imidazoles was accomplished using alcohols as alkylating agents in the presence of a [Cp*IrCl2]2/K2CO3 system. The iridium-catalyzed regioselective reaction is simple, efficient, general, and environmentally benign. Copyright
Copper-catalyzed synthesis of 2-aminobenzimidazoles from carbonimidoyl dichlorides and amines
Yu, Hui,Liu, Qiong,Li, Yuzhe,Ni, Chongzhi
, p. 5253 - 5256 (2012/10/30)
A new protocol for the synthesis of a variety of 2-aminobenzimidazole derivatives has been developed. O-haloaryl carbonimidoyl dichloride reacted with anilines to generate an o-haloaryl guanidine intermediate, which underwent copper catalyzed ring closure to afford 2-aminobenzimidazole derivative in moderate yields.
