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

Improved Synthesis and Crystal Structure of Dalcetrapib

1,* , 2
,
3
,
3
 and
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 / Revised: 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 CETP inhibitor; dalcetrapib; disulfide; thioester
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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

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