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

Improved Synthesis and Crystal Structure of Dalcetrapib

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Received: 15 August 2012; in revised form: 5 September 2012 / Accepted: 14 September 2012 / Published: 19 October 2012
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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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