A Three-Step Synthesis of Acotiamide for the Treatment of Patients with Functional Dyspepsia was written by Fu, Kai;Yang, Liu;Wang, Qiu-Fen;Zhan, Fu-Xu;Wang, Bin;Yang, Qian;Ma, Zhi-Jia;Zheng, Geng-Xiu. And the article was included in Organic Process Research & Development in 2015.Electric Literature of C5H6ClN This article mentions the following:
A three-step synthesis of acotiamide is described. The agent is marketed in Japan for treatment of patients with functional dyspepsia. We designed a one-pot method to prepare the key intermediate I from 2,4,5-trimethoxybenzoic acid via an acyl chloride and amide and then reacted with H2NCH2CH2N(iPr)2 to obtain acotiamide under solvent-free condition. With the use of DCC, an unavoidable impurity was also successfully converted into the desired acotiamide. After isolation of acotiamide, we carried forward to the next step of HCl salt formation, which proved to be a very effective procedure for the removal of practically all major impurities. The process is cost-effective, simple to operate, and easy to scale-up. In the experiment, the researchers used many compounds, for example, Pyridinehydrochloride (cas: 628-13-7Electric Literature of C5H6ClN).
Pyridinehydrochloride (cas: 628-13-7) belongs to pyridine derivatives. Pyridine is diamagnetic and has a diamagnetic susceptibility of â?8.7 à 10â? cm3·molâ?.The molecular electric dipole moment is 2.2 debyes. The standard enthalpy of formation is 100.2 kJ·molâ? in the liquid phase and 140.4 kJ·molâ? in the gas phase. Pyridine derivatives are also useful as small-molecule α-helix mimetics that inhibit protein-protein interactions, as well as functionally selective GABA ligands.Electric Literature of C5H6ClN