Synthesis of Vixotrigine, a Voltage- and Use-Dependent Sodium Channel Blocker. Part 2: Development of a Late-Stage Process was written by Chen, Robbie;Couming, Vincent;Guzowski, John Jr.;Irdam, Erwin;Kiesman, William F.;Kwok, Daw-Iong Albert;Liang, Wenli;Mack, Tamera;O’Brien, Erin M.;Opalka, Suzanne M.;Patience, Daniel;Sahli, Stefan;Walker, Donald G.;Osei-Yeboah, Frederick;Gu, Chaozhan;Zhang, Xin;Stockli, Markus;Stucki, Thiemo;Matzinger, Hanspeter;Kuhn, Roman;Thut, Michael;Grohmann, Markus;Haefner, Benjamin;Lotz, Joerg;Nonnenmacher, Michael;Cerea, Paolangelo. And the article was included in Organic Process Research & Development in 2020.HPLC of Formula: 103-16-2 The following contents are mentioned in the article:
As vixotrigine (I·HCl) entered a later clin. phase for trigeminal neuralgia, the development of a sustainable late-stage process was required to meet the supply needs for formulation optimization, phase 3 clin. trials, and registration stability batches (this is the expected com. formulation). In this article, authors describe how the process was streamlined from the early supply route and a comprehensive control strategy was established. Process improvements included improving safety and scalability for a temperature-sensitive Grignard reaction, simplifying unit operations, removal of heterogenous conditions, and route redesign to afford a high yielding, one-pot sequential alkylation and amidation. Improvement in the salt formation step, combined with wet milling, resulted in improved particle properties with enhanced flow properties of the final active pharmaceutical ingredient. The process mass intensity was improved 65% while maintaining drug substance purity at more than 99.8%. This new process has been scaled up to generate metric ton quantities of drug substance. This study involved multiple reactions and reactants, such as 4-Benzyloxyphenol (cas: 103-16-2HPLC of Formula: 103-16-2).
4-Benzyloxyphenol (cas: 103-16-2) belongs to ethers. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits. Cyclic esters are called lactones, regardless of whether they are derived from an organic or inorganic acid. One example of an organic lactone is γ-valerolactone.HPLC of Formula: 103-16-2
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem