23082-50-0Relevant articles and documents
Manufacturing Development and Genotoxic Impurity Control Strategy of the Hedgehog Pathway Inhibitor Vismodegib
Angelaud, Remy,Reynolds, Mark,Venkatramani, Cadapakam,Savage, Scott,Trafelet, Huldreich,Landmesser, Thomas,Demel, Peter,Levis, Michael,Ruha, Olivier,Rueckert, Baerbel,Jaeggi, Heinz
, p. 1509 - 1519 (2016/08/30)
The development work toward the robust and efficient manufacturing process to vismodegib, the active pharmaceutical ingredient (API) in Erivedge, is described. The optimization of the four-stage manufacturing process was designed to produce the API with the required critical quality attributes: (1) the selective catalytic hydrogenation reduction of the nitro compound 3 to the corresponding aniline 4 while minimizing the formation of potential genotoxic (mutagenic) impurities; (2) the control of the polymorphic phase and multipoint specification for particle size distribution.
Benzenesulphonamide derivatives, preparation thereof and therapeutical uses thereof
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, (2008/06/13)
Benzenesulphonamide compounds of general formula (I), wherein R1is a hydrogen or halogen atom such as chlorine or fluorine, or a straight or branched C1-4alkyl or C1-4alkoxy group, each of R2, R3and R4, which are the same or different, is a hydrogen atom or a straight, branched or cyclic C1-4alkyl group, and R1is a hydrogen atom or a C1-2alkyl, C1-2fluoroalkyl or C1-2perfluoroalkyl group, in the form of enantiomers, diastereoisomers or mixtures thereof, including racemic mixtures, as well as pharmaceutically acceptable acid addition salts thereof, are provided for therapeutical use.
Process for the production of nitro derivatives of aromatic compounds
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, (2008/06/13)
Nitroderivates of aromatic compounds which are difficult to nitrate, can readily be obtained by nitration providing that the aromatic compound is treated with nitric acid or another nitrating agent in the presence of aliphatic or cycloaliphatic hydrocarbons monosubstituted or polysubstituted by halogen, the nitro group or an alkyl sulphonyl group, and the nitro derivative formed subsequently isolated.