1. Chiral preparative SFC
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Emmanuelle Lipka
Abstract
Since 1992, the US Food & Drug Administration (FDA) has requested the assessment of each enantiomer pharmacological activity? for racemic drugs and has promoted the development of new chiral drugs as single enantiomers, resulting in the increase of the development of pure ones. Thus in 2017, 3 of 4 top-selling small-molecule drugs were chiral compounds and all of them were pure enantiomers. Consequently, the preparation of pure enantiomer is now a key step for the development of a new drug. Up until recently, preparative liquid chromatography was the method of choice for chiral separation both during the drug discovery phase, to get a few grams, and for the clinical trials requiring kilograms of pure enantiomers. However, the emergence of the Supercritical Fluid Chromatography (SFC) in the 1990s has changed things. Indeed, the preparative SFC offers many advantages including high productivity thanks to high flow rate and short equilibration time as well as low solvent consumption compared to liquid chromatography. Nowadays, SFC is becoming the primary method for preparative chiral chromatography.
Abstract
Since 1992, the US Food & Drug Administration (FDA) has requested the assessment of each enantiomer pharmacological activity? for racemic drugs and has promoted the development of new chiral drugs as single enantiomers, resulting in the increase of the development of pure ones. Thus in 2017, 3 of 4 top-selling small-molecule drugs were chiral compounds and all of them were pure enantiomers. Consequently, the preparation of pure enantiomer is now a key step for the development of a new drug. Up until recently, preparative liquid chromatography was the method of choice for chiral separation both during the drug discovery phase, to get a few grams, and for the clinical trials requiring kilograms of pure enantiomers. However, the emergence of the Supercritical Fluid Chromatography (SFC) in the 1990s has changed things. Indeed, the preparative SFC offers many advantages including high productivity thanks to high flow rate and short equilibration time as well as low solvent consumption compared to liquid chromatography. Nowadays, SFC is becoming the primary method for preparative chiral chromatography.
Kapitel in diesem Buch
- Frontmatter I
- Preface V
- Contents VII
- List of Contributors IX
- 1. Chiral preparative SFC 1
- 2. Supercritical fluid chromatography in bioanalysis 33
- 3. Ultrafast supercritical fluid chromatography 77
- 4. SFC applications for active pharmaceutical ingredient analysis 93
- 5. Analysis of terpenes (mono-, sesqui-, di-, and triterpenes) by SFE and SFC-MS 113
- 6. Synthesis in supercritical carbon dioxide 127
- 7. Applications of supercritical fluid chromatography in the field of edible lipids 163
- Index 189
Kapitel in diesem Buch
- Frontmatter I
- Preface V
- Contents VII
- List of Contributors IX
- 1. Chiral preparative SFC 1
- 2. Supercritical fluid chromatography in bioanalysis 33
- 3. Ultrafast supercritical fluid chromatography 77
- 4. SFC applications for active pharmaceutical ingredient analysis 93
- 5. Analysis of terpenes (mono-, sesqui-, di-, and triterpenes) by SFE and SFC-MS 113
- 6. Synthesis in supercritical carbon dioxide 127
- 7. Applications of supercritical fluid chromatography in the field of edible lipids 163
- Index 189
