19417-90-4Relevant academic research and scientific papers
Isolation and characterization of process related substances of an antipsychotic drug: Iloperidone
Kilaru, Ravendra Babu,Kuruva, Chandra Sekhar,Katla, Venkata Ramana,Chamarthi, Naga Raju
, p. 5307 - 5310 (2013)
Seven unknown recurring impurities were isolated during the synthesis of Iloperidone process. All six impurities were subsequently synthesized and characterized by FTIR, MS and NMR spectral data. The structures of impurities were confirmed as 1-[4-(3-chloropropoxy)-3-methoxyphenyl]ethanone (4), 1-[4-(3-hydroxypropoxy)-3-methoxy phenyl]ethanone (7), 1-[4-(3-bromopropoxy)-3- methoxyphenyl] ethanone (9), 1,1'-[4,4'-(propane-1,3-diylbis(oxy))bis(3-methoxy- 4,1-phenylene)]diethanone (10), 1-[3-(4-acetyl-2-methoxyphenoxy)-propyl]-4-(6- fluorobenzo[d]isoxazol-3-yl)piperidine-1-oxide (11) and in final other two impurities 1-(4-hydroxy-3-methoxyphenyl)-ethanone (2) and 6-fluoro-3-(piperidin- 4-yl)benzo[d]isoxazole (5). The present work describes the formation, synthesis and characterization of these impurities.
Improved and efficient process for the production of highly pure iloperidone: A psychotropic agent
Solanki, Pavankumar V.,Uppelli, Sekhar Babu,Pandit, Bhushan S.,Mathad, Vijayavitthal T.
, p. 342 - 348 (2014/03/21)
The present work describes an improved and highly efficient process for the synthesis of iloperidone (1), an antipsychotic agent, which is free from potential impurities. The synthesis comprises N-alkylation of 1-(4-(3-chloropropoxy)-3-methoxyphenyl)ethanone (4) with 6-fluoro-3-piperidin-4- yl-1,2-benzisoxazole hydrochloride (5) in a mixture of water and heptane as solvent and sodium hydroxide as a base in the presence of tetrabutylammonium bromide as a phase transfer catalyst to yield iloperidone (1) with a yield of around 95% and a purity of 99.80% by HPLC. The present work also describes the optimization details performed to achieve the process attributes responsible for high yield and purity.
