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The utility of sulfonate salts in drug development.
This review sets out to define some of the advantages provided through utilization of sulfonic acids, explaining the importance of their retention as part of a thorough salt selection process. Expand
Mechanism and Processing Parameters Affecting the Formation of Methyl Methanesulfonate from Methanol and Methanesulfonic Acid: An Illustrative Example for Sulfonate Ester Impurity Formation
Sulfonate salts offer useful modification of physicochemical properties of active pharmaceutical ingredients (APIs) containing basic groups, but there are regulatory concerns over the presence ofExpand
Development and validation of an automated static headspace gas chromatography-mass spectrometry (SHS-GC-MS) method for monitoring the formation of ethyl methane sulfonate from ethanol and methane
An automated sample preparation and analysis procedure was developed to monitor the formation of ethyl methane sulfonate from reaction mixtures containing ethanol and methane sulfonic acid, achieving excellent linearity, repeatability and robustness, allowing the system to be used in kinetic studies. Expand
Development of a Manufacturing Process for Sibenadet Hydrochloride, the Active Ingredient of Viozan
A process for commercial manufacture of the dual D2-β2 receptor agonist sibenadet hydrochloride has been developed. The process relies upon introduction of operationally simple chemistry at the finalExpand
A Detailed Study of Sulfonate Ester Formation and Solvolysis Reaction Rates and Application toward Establishing Sulfonate Ester Control in Pharmaceutical Manufacturing Processes
Sulfonate esters of lower alcohols possess the capacity to react with DNA and cause mutagenic events, which in turn may be cancer inducing. Consequently, the control of residues of such substances inExpand
Synthesis of 24xi, 25-dihydroxyprovitamin D3.
The known C-22 aldehyde obtained by degradation of ergosterol acetate (in which the ring B diene system has been protected by Diels–Alder addition of 4-phenyl-1,2,4-triazoline-3,5-dione) undergoesExpand
The formation of acylimino-derivatives of indoles and pyrroles by reactions with nitrilium salts
Abstract N -Methylnitrilium fluoroborates are prepared rapidly by warming trimethyloxonium fluoroborate with a slight excess of the nitrile, subsequent addition of indoles and pyrroles at lowExpand
Synthesis of 25-hydroxyprovitamin D3 and 25xi, 26-dihydroxyprovitamin D3.
The known C-22 aldehyde derived by degradation of ergosterol (in which the ring B diene system has been protected by reaction with 4-phenyl-1,2,4-triazoline-3,5-dione) reacts with the Grignard reagent derived from 4-chloro-2-methylbut-1-ene to give provitamins D3 hydroxylated or at C-25 and C-26. Expand
Enzymatic synthesis of a series of alkyl esters using novozyme 435 in a packed-bed, miniaturized, continuous flow reactor
Using lipase catalysed, enzymatic esterification as a model reaction, we successfully demonstrate the use of miniaturized technology for biocatalytic reactions. Benchmarked against batch reactions,Expand
Photolytic production of vitamin D. The preparative value of a photo-sensitiser
Fluorenone, previously known to sensitise photolytic interconversion of previtamin D and tachysterol trimethylsilyl ethers, is used in a convenient and practical method of increasing the yield ofExpand