A New Solvent System (Cyclopentyl Methyl Ether–Water) in Process Development of Darifenacin HBr

Darifenacin is a potent and competitive M₃ selective receptor antagonist (M₃SRA), and its hydrobromide salt (<b>1</b>) is the active ingredient of pharmaceutical formulations for oral treatment of urinary incontinence. The present work demonstrates an efficient, commercial manufacturing process for darifenacin hydrobromide (<b>1</b>)

Efficient Synthesis of Impurity-C of Antimigraine Agent Rizatriptan Benzoate

During the commercial manufacturing of antimigraine drug Rizatriptan benzoate, several impurities are reported to be formed. This present work demonstrates a convergent and short synthesis of the most critical impurity (C) of Rizatriptan, [2-(5-((1H-1,2,4-triazol-1-yl)­methyl)-1H-indole-2-yl)-<i>N</i>,<i>N</i>-dimethylethanamine (<b>1</b>)], recently reported in U.S. Pharmacopeia

Process Development of Citalopram/Escitalopram Oxalate: Isolation and Synthesis of Novel Impurities

During process optimization of Escitalopram oxalate novel impurities, <b>6</b> and <b>7</b> were observed, which were isolated and characterized, and the proposed structure was confirmed by chemical synthesis. Investigation of the cause of impurities formation improved the yield and purity of the drug product during the bulk API synthesis

14-Membered Macrocyclic Ring-Derived Toolbox: The Identification of Small Molecule Inhibitors of Angiogenesis and Early Embryo Development in Zebrafish Assay

A highly practical and modular synthesis to obtain a diverse 14-membered ring-based macrocyclic toolbox is achieved. These compounds were further tested in zebrafish assays related to early embryonic development, angiogenesis, and neurogenesis, respectively. <b>1.4c</b> was identified as an antiangiogenesis agent

An Efficient, Scalable Process for Benzphetamine Hydrochloride

Commercial manufacturing of benzphetamine hydrochloride along with its impurity profiling is disclosed. Deoxygenation of pseudoephedrine is reported with ∼100% retention by shielding the amine group as its <i>tert</i>-butyl carbamate, which is very straightforward to eliminate at the end. Four unknown process-related impurities are isolated from the samples of final API and characterized on the basis of their NMR and mass spectral analysis. Structures of the isolated impurities are confirmed by independent syntheses and coinjecting with the isolated one

Commercial Manufacturing of Propofol: Simplifying the Isolation Process and Control on Related Substances

A commercially viable manufacturing process for propofol (<b>1</b>) is described. The process avoids acid–base neutralization events during isolation of intermediate, 2,6-di-isopropylbenzoic acid (<b>3</b>) and crude propofol, and thus simplifies the synthesis on industrial scale to a considerable extent. Syntheses of five impurities/related substances (USP and EP) are also described