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• Laus, G
• Kahlenberg, V
• Richter, F
• Nerdinger, S
• Schottenberger, H
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• Laus, G
• Kahlenberg, V
• Richter, F
• Nerdinger, S
• Schottenberger, H
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• Kahlenberg, V
• Richter, F
• Nerdinger, S
• Schottenberger, H

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Crystals 2012, 2(4), 1455-1459; doi:10.3390/cryst2041455

Article

Improved Synthesis and Crystal Structure of Dalcetrapib

Gerhard Laus ^1,* , Volker Kahlenberg ² , Frank Richter ³ , Sven Nerdinger ³  and Herwig Schottenberger ¹

¹ Faculty of Chemistry and Pharmacy, University of Innsbruck, 6020 Innsbruck, Austria ² Institute of Mineralogy and Petrography, University of Innsbruck, 6020 Innsbruck, Austria ³ Sandoz GmbH, 6250 Kundl, Austria

* Author to whom correspondence should be addressed.

Received: 15 August 2012; in revised form: 5 September 2012 / Accepted: 14 September 2012 / Published: 19 October 2012

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Abstract: An improved synthesis of the Cholesteryl Ester Transfer Protein inhibitor dalcetrapib is reported. The precursor disulfide was reduced (a) by Mg/MeOH or (b) by EtSH/DBU/THF. The resulting thiol was acylated (a) by a known procedure or (b) in a one-pot process. Impurities were removed (a) by dithiothreitol (DTT) or (b) by oxidation using H₂O₂. Dalcetrapib crystallized in space group P2₁/c.

Keywords: CETP inhibitor; dalcetrapib; disulfide; thioester

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