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Improved Synthesis and Crystal Structure of Dalcetrapib
Faculty of Chemistry and Pharmacy, University of Innsbruck, 6020 Innsbruck, Austria
Institute of Mineralogy and Petrography, University of Innsbruck, 6020 Innsbruck, Austria
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
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.
Laus G, Kahlenberg V, Richter F, Nerdinger S, Schottenberger H. Improved Synthesis and Crystal Structure of Dalcetrapib. Crystals. 2012; 2(4):1455-1459.
Laus, Gerhard; Kahlenberg, Volker; Richter, Frank; Nerdinger, Sven; Schottenberger, Herwig. 2012. "Improved Synthesis and Crystal Structure of Dalcetrapib." Crystals 2, no. 4: 1455-1459.