Next Article in Journal
Pressure Effect on Organic Conductors
Previous Article in Journal
Determination of the Absolute Configuration of Aegelinol by Crystallization of Its Inclusion Complex with β-Cyclodextrin
Crystals 2012, 2(4), 1455-1459; doi:10.3390/cryst2041455

Improved Synthesis and Crystal Structure of Dalcetrapib

1,* , 2
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
View Full-Text   |   Download PDF [252 KB, uploaded 19 October 2012]   |   Browse Figures


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) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Supplementary material

Share & Cite This Article

Further Mendeley | CiteULike
Export to BibTeX |
EndNote |
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.

View more citation formats

Related Articles

Article Metrics

For more information on the journal, click here


[Return to top]
Crystals EISSN 2073-4352 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert