886372-07-2Relevant academic research and scientific papers
Selective Halogenation of Pyridines Using Designed Phosphine Reagents
Alegre-Requena, Juan V.,Levy, Jeffrey N.,Liu, Renrong,McNally, Andrew,Paton, Robert S.
supporting information, p. 11295 - 11305 (2020/07/13)
Halopyridines are key building blocks for synthesizing pharmaceuticals, agrochemicals, and ligands for metal complexes, but strategies to selectively halogenate pyridine C-H precursors are lacking. We designed a set of heterocyclic phosphines that are installed at the 4-position of pyridines as phosphonium salts and then displaced with halide nucleophiles. A broad range of unactivated pyridines can be halogenated, and the method is viable for late-stage halogenation of complex pharmaceuticals. Computational studies indicate that C-halogen bond formation occurs via an SNAr pathway, and phosphine elimination is the rate-determining step. Steric interactions during C-P bond cleavage account for differences in reactivity between 2- and 3-substituted pyridines.
Synthesis of 4-((1H-benzo[d]imidazol-2-yl)oxy)-3-methylpicolinic acid, a key related substance of Rabeprazole sodium
Bao, Xuefei,Chang, Yan,Chen, Guoliang,He, Xiaoyan,Liu, Zi'ao,Lu, Xiuhong
supporting information, (2020/07/03)
4-((1H-benzo[d]imidazol-2-yl)oxy)-3-methylpicolinic acid (11) is a key related substance of Rabeprazole sodium. In this article, this key related substance is synthesized by using 3-methylpicolinonitrile as a starting material via a five-step processes. By converting 3-methylpicolinonitrile to 4-hydroxy-3-methylpicolinonitrile (13), the preparation of TM becomes practical. This work provides a guarantee for quality standard establishment of Rabeprazole sodium.
INHIBITORS OF PLASMA KALLIKREIN AND USES THEREOF
-
, (2019/09/30)
The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
A simple procedure for the preparation of 2-cyano-4-chloropyridines
Veerareddy, Arava,Surendrareddy, Gogireddy,Dubey
experimental part, p. 961 - 964 (2011/09/16)
Figure represented. 4-Nitro-pyridine-N-oxides are reacted with ethylchloroformate and trimethylsilyl cyanide to give 4-chloro-2-cyanopyridine.
