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

Improved Synthesis and Crystal Structure of Dalcetrapib

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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MDPI and ACS Style

Laus, G.; Kahlenberg, V.; Richter, F.; Nerdinger, S.; Schottenberger, H. Improved Synthesis and Crystal Structure of Dalcetrapib. Crystals 2012, 2, 1455-1459.

AMA Style

Laus G, Kahlenberg V, Richter F, Nerdinger S, Schottenberger H. Improved Synthesis and Crystal Structure of Dalcetrapib. Crystals. 2012; 2(4):1455-1459.

Chicago/Turabian Style

Laus, Gerhard; Kahlenberg, Volker; Richter, Frank; Nerdinger, Sven; Schottenberger, Herwig. 2012. "Improved Synthesis and Crystal Structure of Dalcetrapib." Crystals 2, no. 4: 1455-1459.

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