Chirality in Drug Research by Francotte E., Lindner W.

By Francotte E., Lindner W.

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S. Venturella, Natural Products, in A. R. , Mack Publishing Company, USA, 1985, p. 418. 34 E. L. Eliel, S. H. Wilen, L. N. Mander, Stereochemistry of Organic Compounds, Wiley-Interscience, USA, 1994, pp. 2–4. -J. Haüy, Traité de Minéralogie, Conseil des Mines, France, 1801. 36 H. Kopp, Geschichte Chem. 1847, 4, 349. -B. Biot, Bull. Soc. Philomatique 1815, 190–192. 38 J. Chautard, Compt. Rend. Acad. Sci. 1853, 37, 166–167. 39 L. Pasteur, Compt. Rend. Acad. Sci. 1848, 34, 535–538. T. Kelvin, J. Oxford Univ.

L. Eliel, S. H. Wilen, L. N. Mander, Stereochemistry of Organic Compounds, Wiley-Interscience, New York, 1994, p. 1194. 4 K. Mislow, Topics Stereochem. 1999, 22, 1. 5 J. Gal, Enantiomer, 1998, 3, 263–273. 6 G. Thomas, Medicinal Chemistry: An Introduction, John Wiley & Sons, Ltd, UK, 2000, p. 3. 7 A. Burger, Introduction: History and Economics of Medicinal Chemistry, in M. E. , John Wiley & Sons, New York, 1980, pp. 7–22. 8 A. Burger, Drugs and People: Medications, Their History and Origins, and the Way They Act, University Press of Virginia, USA, 1986, p.

Instead, in 1966–1968, the major focus became homogenous counterparts, an area in which the research groups of Nozaki [21], Horner [22], and Knowles [6, 8] have made a lasting imprint with their landmark preparation of metal complexes using different chiral phosphines as ligands. Optical purities gained early on were low (< 15 %), but the situation improved rapidly, driven by the discovery of the DIOP ligand by Kagan [23] around 1970. This breakthrough opened up the versatile area of C2 symmetric biphosphines and was instrumental for the launch of l-Dopa production a few years later, where an outstanding quality of up to 95 % ee was achieved – a value that still compares favorably with many processes developed much more recently.

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